Simon L Croft

Summary

Affiliation: Drugs for Neglected Diseases Initiative
Country: Switzerland

Publications

  1. ncbi Public-private partnership: from there to here
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, 1 place Saint Gervais, 1201 Geneva, Switzerland
    Trans R Soc Trop Med Hyg 99:S9-14. 2005
  2. ncbi Current scenario of drug development for leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, Geneva, Switzerland
    Indian J Med Res 123:399-410. 2006
  3. pmc Drug resistance in leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative, 1 place Saint Gervais, CH 1201 Geneva, Switzerland
    Clin Microbiol Rev 19:111-26. 2006
  4. ncbi Chemotherapy of trypanosomiases and leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative, 1 place Saint Gervais, CH 1201 Geneva, Switzerland
    Trends Parasitol 21:508-12. 2005
  5. ncbi Miltefosine--discovery of the antileishmanial activity of phospholipid derivatives
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, 1 Place St Gervais, CH 1201 Geneva, Switzerland
    Trans R Soc Trop Med Hyg 100:S4-8. 2006
  6. ncbi Leishmaniasis--current chemotherapy and recent advances in the search for novel drugs
    Simon L Croft
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Trends Parasitol 19:502-8. 2003
  7. pmc Toxicity and antileishmanial activity of a new stable lipid suspension of amphotericin B
    Malika Larabi
    Laboratoire de Physico chimie, Pharmacotechnie et Biopharmacie, UMR CNRS 8612, Faculte de Pharmacie, Universite Paris XI, 92296 Chatenay Malabry Cedex, France
    Antimicrob Agents Chemother 47:3774-9. 2003
  8. ncbi In-vitro and in-vivo studies on a topical formulation of sitamaquine dihydrochloride for cutaneous leishmaniasis
    Tracy Garnier
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, UK
    J Pharm Pharmacol 58:1043-54. 2006
  9. ncbi Mechanisms of experimental resistance of Leishmania to miltefosine: Implications for clinical use
    F Javier Pérez-Victoria
    Instituto de Parasitologia y Biomedicina Lopez Neyra, Spanish Research Council C S I C, Technological Park of Health Sciences, Avda del Conocimiento s n, 18100 Armilla, Granada, Spain
    Drug Resist Updat 9:26-39. 2006
  10. ncbi Synthesis, in vitro evaluation, and antileishmanial activity of water-soluble prodrugs of buparvaquone
    Antti Mäntylä
    Department of Pharmaceutical Chemistry, University of Kuopio, PO Box, 1627, FIN 70211 Kuopio, Finland
    J Med Chem 47:188-95. 2004

Collaborators

Detail Information

Publications61

  1. ncbi Public-private partnership: from there to here
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, 1 place Saint Gervais, 1201 Geneva, Switzerland
    Trans R Soc Trop Med Hyg 99:S9-14. 2005
    ..The challenge is to ensure that the products are delivered to the people who need them and to ensure that scientists in endemic countries are involved in the whole process...
  2. ncbi Current scenario of drug development for leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, Geneva, Switzerland
    Indian J Med Res 123:399-410. 2006
    ..The process for discovery and development of new antileishmanials would also benefit from improved models, for example, transfected parasites, and non invasive methods of measuring parasite load in rodent models of infection...
  3. pmc Drug resistance in leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative, 1 place Saint Gervais, CH 1201 Geneva, Switzerland
    Clin Microbiol Rev 19:111-26. 2006
    ....
  4. ncbi Chemotherapy of trypanosomiases and leishmaniasis
    Simon L Croft
    Drugs for Neglected Diseases Initiative, 1 place Saint Gervais, CH 1201 Geneva, Switzerland
    Trends Parasitol 21:508-12. 2005
    ..Financial constraints continue to represent a major hurdle to drug development. However, the appearance of not-for-profit product-development partnerships offers a new paradigm for bringing new drugs to patients...
  5. ncbi Miltefosine--discovery of the antileishmanial activity of phospholipid derivatives
    Simon L Croft
    Drugs for Neglected Diseases Initiative DNDi, 1 Place St Gervais, CH 1201 Geneva, Switzerland
    Trans R Soc Trop Med Hyg 100:S4-8. 2006
    ..Miltefosine is active against most Leishmania species, including those that cause cutaneous disease...
  6. ncbi Leishmaniasis--current chemotherapy and recent advances in the search for novel drugs
    Simon L Croft
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Trends Parasitol 19:502-8. 2003
  7. pmc Toxicity and antileishmanial activity of a new stable lipid suspension of amphotericin B
    Malika Larabi
    Laboratoire de Physico chimie, Pharmacotechnie et Biopharmacie, UMR CNRS 8612, Faculte de Pharmacie, Universite Paris XI, 92296 Chatenay Malabry Cedex, France
    Antimicrob Agents Chemother 47:3774-9. 2003
    ..It was unable to reverse the resistance of an AMB-resistant L. donovani strain. In vivo LC-AMB was less efficient than AmBisome against L. donovani...
  8. ncbi In-vitro and in-vivo studies on a topical formulation of sitamaquine dihydrochloride for cutaneous leishmaniasis
    Tracy Garnier
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, UK
    J Pharm Pharmacol 58:1043-54. 2006
    ..Several formulations were tested in-vivo against Leishmania major cutaneous lesions in BALB/c mice. None of the sitamaquine dihydrochloride formulations tested appeared to either slow lesion progression or reduce parasite burden...
  9. ncbi Mechanisms of experimental resistance of Leishmania to miltefosine: Implications for clinical use
    F Javier Pérez-Victoria
    Instituto de Parasitologia y Biomedicina Lopez Neyra, Spanish Research Council C S I C, Technological Park of Health Sciences, Avda del Conocimiento s n, 18100 Armilla, Granada, Spain
    Drug Resist Updat 9:26-39. 2006
    ....
  10. ncbi Synthesis, in vitro evaluation, and antileishmanial activity of water-soluble prodrugs of buparvaquone
    Antti Mäntylä
    Department of Pharmaceutical Chemistry, University of Kuopio, PO Box, 1627, FIN 70211 Kuopio, Finland
    J Med Chem 47:188-95. 2004
    ..In addition, 4b easily released the parent drug in human skin homogenate and, therefore, is a promising prodrug candidate to deliver buparvaquone through the skin for the treatment of cutaneous leishmaniasis...
  11. pmc Novel azasterols as potential agents for treatment of leishmaniasis and trypanosomiasis
    Silvia Orenes Lorente
    Welsh School of Pharmacy, Cardiff University, Cardiff, CF10 3XF, United Kingdom
    Antimicrob Agents Chemother 48:2937-50. 2004
    ..The compounds were also found to be active against the bloodstream form (trypomastigotes) of Trypanosoma brucei rhodesiense, a causative agent of African trypanosomiasis...
  12. ncbi In vitro antiprotozoal and cytotoxic activities of some alkaloids, quinones, flavonoids, and coumarins
    Maria del Rayo Camacho
    Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, London, UK
    Planta Med 70:70-2. 2004
  13. ncbi Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa
    Silvia Orenes Lorente
    Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, UK
    Bioorg Med Chem 13:3519-29. 2005
    ..Some compounds also showed growth inhibition of T. brucei rhodesiense trypomastigotes, although in this case alternative modes of action other than inhibition of SQS are probably involved...
  14. pmc Antiparasitic activities and toxicities of individual enantiomers of the 8-aminoquinoline 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3,4-dichlorophenoxy]quinoline succinate
    N P Dhammika Nanayakkara
    National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA
    Antimicrob Agents Chemother 52:2130-7. 2008
    ....
  15. ncbi The sensitivity of clinical isolates of Leishmania from Peru and Nepal to miltefosine
    Vanessa Yardley
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom
    Am J Trop Med Hyg 73:272-5. 2005
    ..If this model can be correlated to therapeutic outcome, it may have implications for the interpretation of clinical trials...
  16. ncbi Antimalarial drug discovery: efficacy models for compound screening
    David A Fidock
    Department of Microbiology and Immunology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, New York 10461, USA
    Nat Rev Drug Discov 3:509-20. 2004
  17. pmc In vitro and in vivo interactions between miltefosine and other antileishmanial drugs
    Karin Seifert
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, United Kingdom
    Antimicrob Agents Chemother 50:73-9. 2006
    ..38). The potentiation of miltefosine in vivo was also achieved with the combination of miltefosine and paromomycin (AEI of up to 7.22)...
  18. ncbi Characterisation of Leishmania donovani promastigotes resistant to hexadecylphosphocholine (miltefosine)
    Karin Seifert
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Int J Antimicrob Agents 22:380-7. 2003
    ..Resistance was stable up to 12 weeks in drug-free culture medium. No amplification of specific genes, including the multidrug resistance P-glycoprotein gene, could be detected in the resistant parasites...
  19. ncbi Chemotherapy of leishmaniasis
    Simon L Croft
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Curr Pharm Des 8:319-42. 2002
    ..In short, there remains a pressing need for new anti-leishmanials and this chapter reviews the current status of chemotherapy, the various avenues being investigated by researchers and their potential application in the future...
  20. ncbi Drug sensitivity of Leishmania species: some unresolved problems
    Simon L Croft
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London, WC1E 7HT, UK
    Trans R Soc Trop Med Hyg 96:S127-9. 2002
    ..Reporter genes and the polymerase chain reaction will improve assays both in vitro and in vivo for the identification and evaluation of new drugs...
  21. ncbi Visceral leishmaniasis: current status of control, diagnosis, and treatment, and a proposed research and development agenda
    Philippe J Guerin
    Norwegian Institute of Public Health, Norway
    Lancet Infect Dis 2:494-501. 2002
    ..This article reviews the current situation and perspectives for diagnosis, treatment, and control of visceral leishmaniasis, and lists some priorities for research and development...
  22. ncbi Sensitivities of Leishmania species to hexadecylphosphocholine (miltefosine), ET-18-OCH(3) (edelfosine) and amphotericin B
    Patricia Escobar
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Acta Trop 81:151-7. 2002
    ..5-37.1 microM against amastigotes. Amphotericin B deoxycholate was used as the standard drug and gave submicromolar ED(50) values in all assays; L. mexicana was the least sensitive species to this drug...
  23. ncbi Inactivation of the miltefosine transporter, LdMT, causes miltefosine resistance that is conferred to the amastigote stage of Leishmania donovani and persists in vivo
    Karin Seifert
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Int J Antimicrob Agents 30:229-35. 2007
    ..90% inhibition in wild-type infections). No cross-resistance to other antileishmanial drugs was observed in M-mutR amastigotes...
  24. pmc Leishmaniasis: new approaches to disease control
    Clive R Davies
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London WC1E 7HT
    BMJ 326:377-82. 2003
  25. ncbi Antiprotozoal activities of phospholipid analogues
    Simon L Croft
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
    Mol Biochem Parasitol 126:165-72. 2003
    ..This review will focus on the biological activities of phospholipid analogues. Biochemical and molecular targets and mechanism(s) of action have been studied extensively in tumor cells but have not been determined in protozoa...
  26. ncbi Artemisone--a highly active antimalarial drug of the artemisinin class
    Richard K Haynes
    Department of Chemistry, Open Laboratory of Chemical Biology, Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, PR China
    Angew Chem Int Ed Engl 45:2082-8. 2006
  27. ncbi Development and validation of RP-HPLC-UV method for simultaneous determination of buparvaquone, atenolol, propranolol, quinidine and verapamil: a tool for the standardization of rat in situ intestinal permeability studies
    Gantala Venkatesh
    Centre for Drug Research, Universiti Sains Malaysia, 11800 Penang, Malaysia
    J Pharm Biomed Anal 43:1546-51. 2007
    ..Stability studies were carried out at different storage conditions and all the analytes were found to be stable. This method is simple, reliable and can be routinely used for accurate permeability characterization...
  28. ncbi Antimalarial compounds from Kniphofia foliosa roots
    Abraham Abebe Wube
    Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Universitaetsplatz 4 1, A 8010 Graz, Austria
    Phytother Res 19:472-6. 2005
    ..This is the first report of the inhibition of the growth of P. falciparum by anthraquinone-anthrone dimers and establishes them as a new class of potential antimalarial compounds with very little host cell toxicity...
  29. ncbi Topical buparvaquone formulations for the treatment of cutaneous leishmaniasis
    Tracy Garnier
    School of Pharmacy, University of Hertfordshire, College Lane, Hatfield AL10 9AB, UK
    J Pharm Pharmacol 59:41-9. 2007
    ....
  30. ncbi Metalloantimalarials: synthesis, X-ray crystal structure of potent antimalarial copper (II) complex of arylazo-4-hydroxy-1,2-naphthoquinone
    Nikhil H Gokhale
    Department of Chemistry, University of Pune, Ganeshkhind Road, Pune 411007, India
    Bioorg Med Chem Lett 16:430-2. 2006
    ..The in vitro antimalarial activity of analogous compounds against Plasmodium falciparum 3D7 strain reveals correlation with metal redox couple, suggesting component of parasitic electron transport chain as a possible target...
  31. doi Anti-malarial efficacy of pyronaridine and artesunate in combination in vitro and in vivo
    Livia Vivas
    London School of Hygiene and Tropical Medicine, Department of Infectious and Tropical Diseases, London WC1E 7HT, United Kingdom
    Acta Trop 105:222-8. 2008
    ..The data suggest that the combination of pyronaridine and artesunate should have potential in areas of multi-drug resistant malaria...
  32. ncbi Inhibition of Trypanosoma cruzi hexokinase by bisphosphonates
    Michael P Hudock
    Department of Biophysics, University of Illinois at Urbana Champaign, 607 South Mathews Avenue, Urbana, Illinois 61801, USA
    J Med Chem 49:215-23. 2006
    ..2 microM IC(50) versus the clinically relevant intracellular amastigote form of T. cruzi, but only a approximately 1-2 mM IC(50) versus Dictyostelium discoideum and a human cell line, indicating selective activity versus T. cruzi...
  33. pmc New azasterols against Trypanosoma brucei: role of 24-sterol methyltransferase in inhibitor action
    Ludovic Gros
    Welsh School of Pharmacy, Cardiff University, UK
    Antimicrob Agents Chemother 50:2595-601. 2006
    ..Likewise, Western blot analysis and activity determinations evidenced the existence of active enzyme in both forms of the parasite. We conclude that the designed compounds act at sites other than 24-SMT in Trypanosoma brucei...
  34. ncbi Neglected diseases: progress in drug development
    Simon L Croft
    Curr Opin Investig Drugs 8:103-4. 2007
  35. pmc Antileishmanial structure-activity relationships of synthetic phospholipids: in vitro and in vivo activities of selected derivatives
    Karin Seifert
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom
    Antimicrob Agents Chemother 51:4525-8. 2007
    ..Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity...
  36. ncbi Metallocene-based antimalarials: an exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum
    Margaret A L Blackie
    Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
    Bioorg Med Chem 15:6510-6. 2007
    ..Unexpectedly high activity for quinoline compounds lacking the 7-chloro substituent suggests the ferrocenyl moiety may have an additive and/or synergistic effect...
  37. doi Optimization and validation of RP-HPLC-UV method with solid-phase extraction for determination of buparvaquone in human and rabbit plasma: application to pharmacokinetic study
    Gantala Venkatesh
    Centre for Drug Research, Universiti Sains Malaysia, 11800 Penang, Malaysia
    Biomed Chromatogr 22:535-41. 2008
    ..Partial validation studies were carried out using rabbit plasma and intra- and inter-day precision and accuracy were within 7%. This method is simple, reliable and can be routinely used for preclinical pharmacokinetic studies for BPQ...
  38. ncbi Preparation of transition-state analogues of sterol 24-methyl transferase as potential anti-parasitics
    Silvia Orenes Lorente
    Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3XF, UK
    Bioorg Med Chem 13:5435-53. 2005
    ..donovani and T. cruzi, but no inhibition of the enzyme. In addition, some of the compounds had anti-proliferative activity against the bloodstream forms of Trypanosoma brucei rhodesiense, which causes African trypanosomiasis...
  39. ncbi Mapping the binding site for gossypol-like inhibitors of Plasmodium falciparum lactate dehydrogenase
    Rebecca Conners
    Department of Biochemistry, University of Bristol, Bristol BS8 1TD, UK
    Mol Biochem Parasitol 142:137-48. 2005
    ....
  40. ncbi Azasterols as inhibitors of sterol 24-methyltransferase in Leishmania species and Trypanosoma cruzi
    Filippo Magaraci
    Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3XF, UK
    J Med Chem 46:4714-27. 2003
    ..However, some azasterols which were not good inhibitors of 24-SMT also showed antiproliferative activity, suggesting that there may be other modes of actions of these compounds...
  41. ncbi Cissampeloflavone, a chalcone-flavone dimer from Cissampelos pareira
    Irama Ramírez
    Faculty of Pharmacy, University of Los Andes, Mérida ZP 5101, Venezuela
    Phytochemistry 64:645-7. 2003
    ..This has been assigned the trivial name cissampeloflavone. The compound has good activity against Trypanosoma cruzi and T. brucei rhodesiense and has a low toxicity to the human KB cell line...
  42. ncbi Structure-activity relationships of antileishmanial and antimalarial chalcones
    Mei Liu
    Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
    Bioorg Med Chem 11:2729-38. 2003
    ..Despite different requirements, two alkoxylated chalcones (8, 19) were identified which combined good antimalarial and antileishmanial activities...
  43. ncbi Antileishmanial activity of two gamma-pyrones from Podolepsis hieracioides (Asteraceae)
    Oliver Kayser
    Institute of Pharmacy Pharmaceutical Technology, Biopharmacy and Biotechnology, Freie Universitat Berlin, Kelchstrasse 31, D 112169 Berlin, Germany
    Acta Trop 86:105-7. 2003
    ..7, SKMel, and KB; IC(50)=11.5->25.0 microg/ml). Both compounds were not active against Trypanosoma cruzi or Trypanosoma br. brucei (IC(50)>30 microg/ml)...
  44. ncbi Synthesis and biological activity of nitro heterocycles analogous to megazol, a trypanocidal lead
    Gérard Chauviere
    Groupe de Chimie Organique Biologique, Laboratoire de Synthèse et Physicochimie de Molécules d Intérêt Biologique, Universite Paul Sabatier, UMR CNRS 5068, 31062 Toulouse, France
    J Med Chem 46:427-40. 2003
    ..The mutagenicity of this compound is at present being reevaluated, and metabolism is also under investigation prior to possible further developments...
  45. ncbi Assessment of the antiprotozoal activity of Galphimia glauca and the isolation of new nor-secofriedelanes and nor-friedelanes
    Maria del Rayo Camacho
    Centre for Pharmacognosy and Phytotherapy, and Department of Pharmaceutical and Biological Chemistry, The School of Pharmacy, University of London, 29 39 Brunswick Square, UK
    J Nat Prod 65:1457-61. 2002
    ..2 microM against Trypanosoma brucei brucei, and 63.8 microM against Leishmania donovani. Quercetin was found to be inactive against KB cells (IC(50) = 295.8 microM)...
  46. ncbi Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid
    Mankil Jung
    Department of Chemistry, Yonsei University, Seoul 120 749, Korea
    J Med Chem 45:4940-4. 2002
    ..66 h, 23 times more stable than clinically useful arteether in simulated stomach acid, and improved solubility, 4 times more soluble than artemisinin in water...
  47. ncbi In vitro activity of Triclisia patens and some bisbenzylisoquinoline alkaloids against Leishmania donovani and Trypanosoma brucei brucei
    Maria del Rayo Camacho
    Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, 29 39 Brunswick Square, London WC 1N 1AX, UK
    Phytother Res 16:432-6. 2002
    ..Thalisopidine showed the strongest activity (IC(50) = 1.14 microM) against Trypanosoma brucei brucei blood stream form trypomastigotes, but was less active than pentamidine...
  48. ncbi Topical treatment for cutaneous leishmaniasis
    Tracy Garnier
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, UK
    Curr Opin Investig Drugs 3:538-44. 2002
    ..The focus of this review is on recent developments in the field of topical treatment for cutaneous leishmaniasis and rational approaches to enhance topical drug absorption...
  49. ncbi Synthesis and in vitro anti-protozoal activity of a series of benzotropolone derivatives incorporating endocyclic hydrazines
    Hongyu Ren
    Department of Chemistry and Biochemistry, University of the Sciences in Philadelphia, 600 South 43rd Street, Philadelphia, PA 19104, USA
    Eur J Med Chem 38:949-57. 2003
    ..cruzi infections. In addition, all but one of the new bicyclic hydrazine esters are virtually non-toxic, one of the most important drawbacks of currently available trypanocidal drugs...
  50. ncbi Targetable water-soluble polymer-drug conjugates for the treatment of visceral leishmaniasis
    Anjan Nan
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD 21201, USA
    J Control Release 94:115-27. 2004
    ..0001) than nontargeted conjugate (47% inhibition). HPMA copolymers containing ManN in the side chains can potentially reduce the toxicity and increase efficacy of anti-leishmanial drugs for the treatment of VL...
  51. ncbi Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo
    Subhash Ghosh
    Department of Chemistry, University of Illinois at Urbana Champaign, 600 South Mathews Avenue, Urbana, Illinois 61801, USA
    J Med Chem 47:175-87. 2004
    ..Taken together, these results show that bisphosphonates appear to be useful lead compounds for the development of novel antiamebic and antimalarial drugs...
  52. ncbi Synthesis of some cryptolepine analogues, assessment of their antimalarial and cytotoxic activities, and consideration of their antimalarial mode of action
    Onyeka Onyeibor
    The School of Pharmacy, Department of Biomedical Sciences and Tom Connors Cancer Research Centre, University of Bradford, West Yorkshire, BD7 1DP, UK
    J Med Chem 48:2701-9. 2005
    ..No correlation was seen (r(2) = 0.0781) suggesting that the potent antimalarial activity of compounds such as 15 involves other mechanisms in addition to the inhibition of hemozoin formation...
  53. ncbi In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability
    Dora Carrico
    Department of Chemistry, Yale University, PO Box 208107, New Haven, CT 06520, USA
    Bioorg Med Chem 12:6517-26. 2004
    ....
  54. ncbi Highly antimalaria-active artemisinin derivatives: biological activity does not correlate with chemical reactivity
    Richard K Haynes
    Department of Chemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, P R China
    Angew Chem Int Ed Engl 43:1381-5. 2004
  55. pmc Inhibitors of Leishmania mexicana CRK3 cyclin-dependent kinase: chemical library screen and antileishmanial activity
    Karen M Grant
    Wellcome Centre for Molecular Parasitology, University of Glasgow, Glasgow, United Kingdom
    Antimicrob Agents Chemother 48:3033-42. 2004
    ..Thus, use of chemical inhibitors supports genetic studies to confirm CRK3 as a validated drug target in Leishmania and provides pharmacophores for further drug development...
  56. ncbi Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents
    Junko Ohkanda
    Department of Chemistry, Yale University, PO Box 208107, New Haven, Connecticut 06520, USA
    J Med Chem 47:432-45. 2004
    ..brucei cells were shown to be highly correlated. These studies validate TbPFT as a target for the development of novel therapeutics against African sleeping sickness...
  57. ncbi Synthesis and antileishmanial activity of novel buparvaquone oxime derivatives
    Antti Mäntylä
    Department of Pharmaceutical Chemistry, University of Kuopio, Finland
    Bioorg Med Chem 12:3497-502. 2004
    ..Further in vivo studies are needed to verify the biological activity of buparvaquone-oximes in the treatment of leishmaniasis...
  58. ncbi Antikinetoplastid activity of 3-aryl-5-thiocyanatomethyl-1,2,4-oxadiazoles
    Denise M Cottrell
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    Bioorg Med Chem 12:2815-24. 2004
    ..doses at 5mg/kg and by 61% when administered orally for 5 days at 50 mg/kg. These results indicate that aromatic thiocyanates hold promise for the treatment of leishmanial infections if the selectivity of these compounds can be improved...
  59. ncbi Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity
    Angus Cameron
    Department of Biochemistry and Molecular Recognition Centre, University of Bristol, Bristol BS8 1TD, United Kingdom
    J Biol Chem 279:31429-39. 2004
    ..In combination these studies also provide strong support for the validity of targeting the Plasmodium glycolytic pathway and, in particular, LDH in the search for novel anti-malarials...
  60. ncbi Prediction of anti-plasmodial activity of Artemisia annua extracts: application of 1H NMR spectroscopy and chemometrics
    Nigel J C Bailey
    SCYNEXIS Europe Ltd, Fyfield Business and Research Park, Fyfield Road, Ongar, Essex CM5 0GS, UK
    J Pharm Biomed Anal 35:117-26. 2004
    ..8. This approach was also able to correlate 1H NMR spectra with cytotoxicity (R2=0.9, Q2=0.8). This work demonstrates the potential of NMR spectroscopy and chemometrics for the development of predictive models of anti-plasmodial activity...
  61. pmc In vivo activities of farnesyl pyrophosphate synthase inhibitors against Leishmania donovani and Toxoplasma gondii
    Vanessa Yardley
    Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London WC1E 7HT, United Kingdom
    Antimicrob Agents Chemother 46:929-31. 2002
    ..donovani by intravenous administration. Risedronate had a 50% effective dosage of five 2.6-mg/kg of body weight intraperitoneal doses against L. donovani-infected mice but was less effective against T. gondii-infected mice...

Research Grants3

  1. Development of a low cost formulation of amphotericin B
    SHING CHANG; Fiscal Year: 2007
    ....
  2. K777 for treatment of Chagas Disease: IND-enabling Studies and IND Submission
    SHING CHANG; Fiscal Year: 2010
    ..This proposal is designed to complete all remaining requirements as agreed with the FDA to allow K777 to move into clinical trials. ..