Research Topics
| Cyrus J BacchiSummaryAffiliation: Pace University Country: USA Publications
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Detail Information
Publications
Trypanocidal activity of 8-methyl-5'-{[(Z)-4-aminobut-2-enyl]-(methylamino)}adenosine (Genz-644131), an adenosylmethionine decarboxylase inhibitorCyrus J Bacchi
Haskins Laboratories, Pace University, 41 Park Row, New York, NY 10038, USA
Antimicrob Agents Chemother 53:3269-72. 2009..This study shows that AdoMetDC remains an attractive chemotherapeutic target in African trypanosomes and that chemical changes in AdoMetDC inhibitors can produce more favorable drug characteristics than the lead compound...
Metabolism of an alkyl polyamine analog by a polyamine oxidase from the microsporidian Encephalitozoon cuniculiCyrus J Bacchi
Haskins Laboratories, Pace University, 41 Park Row, New York, NY 10038, USA
Antimicrob Agents Chemother 53:2599-604. 2009..cuniculi. The results in this study demonstrate competitive inhibition of oxidase activity by BW-1 and support further studies of this oxidase activity by the parasite and host...
Polyamine metabolism in a member of the phylum Microspora (Encephalitozoon cuniculi): effects of polyamine analoguesCyrus J Bacchi
Department of Biology, Pace University, New York, NY 10038, USA
Microbiology 150:1215-24. 2004..The interest in Enc. cuniculi polyamine metabolism and the biochemical effects of these polyamine analogues is warranted since they cure model infections of Enc. cuniculi in mice and are potential candidates for human clinical trials...
Polyamine metabolism in the MicrosporidiaC J Bacchi
Department of Biology, Pace University, New York, NY 10038, U S A
Biochem Soc Trans 31:420-3. 2003..In light of enhanced polyamine uptake in Enc. cuniculi, we have begun to study bis-aryl 3-7-3 and bis-ethyl oligoamine analogues as leads for chemotherapy of microsporidia...
Polyamine metabolism as chemotherapeutic target in protozoan parasitesC J Bacchi
Haskins Laboratories and Department of Biology, Pace University, 41 Park Row, New York, NY 10038, USA
Mini Rev Med Chem 2:553-63. 2002..Approaches include development of mono- and di-substituted polyamine analogs targeting polyamine interconversion, as well as more traditional targeting of synthetic enzymes and related pathways...
Novel synthetic polyamines are effective in the treatment of experimental microsporidiosis, an opportunistic AIDS-associated infectionCyrus J Bacchi
Haskins Laboratories and Department of Biology, Pace University, New York, New York 10038 1598, USA
Antimicrob Agents Chemother 46:55-61. 2002..25 to 5 mg/kg of body weight/day for a total of 10 days. Cured animals demonstrated no evidence of parasitemia by either PCR or histologic staining of tissues 30 days after untreated control animals died...
Polyamine synthesis and interconversion by the Microsporidian Encephalitozoon cuniculiC J Bacchi
Haskins Laboratory, Pace University, New York, New York 10038, USA
J Eukaryot Microbiol 48:374-81. 2001..Pre-emergent spores were metabolically active with respect to polyamine synthesis and interconversion, while intact mature spores harvested from culture supernatants had little metabolic activity...
In situ kinetic characterization of methylthioadenosine transport by the adenosine transporter (P2) of the African Trypanosoma brucei brucei and Trypanosoma brucei rhodesienseB Goldberg
Department of Biology, St Francis College, 180 Remsen Street, Brooklyn Heights, 11201, Brooklyn, NY, USA
Biochem Pharmacol 61:449-57. 2001..The significant ability of African trypanosomes to transport MTA and related intermediates is an important consideration in the design and development of selective chemotherapeutic agents...
In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitorsC J Bacchi
Haskins Laboratories, Pace University, New York, New York 10038, USA
Antimicrob Agents Chemother 40:1448-53. 1996....
Metabolic effects of a methylthioadenosine phosphorylase substrate analog on African trypanosomesC J Bacchi
Department of Biology, Pace University, New York, NY 10038 1502, USA
Biochem Pharmacol 57:89-96. 1999..Thus, HETA interferes with a series of biochemical events involving the participation of AdoMet and methionine in polyamine synthesis, protein synthesis, and transmethylation reactions...
Antitrypanosomal activity of a new triazine derivative, SIPI 1029, In vitro and in model infectionsC J Bacchi
Haskins Laboratories, Pace University, New York, New York 10038, USA
Antimicrob Agents Chemother 42:2718-21. 1998..The activity of SIPI 1029 in this study indicates that this class of compounds (diaminotriazines) should be explored as leads for new human and veterinary trypanocides...
Protein methylases in Trypanosoma brucei brucei: activities and response to DL-alpha-difluoromethylornithineN Yarlett
Haskins Laboratories, Department of Biology, Pace University, New York, NY 10038
J Gen Microbiol 137:717-24. 1991..The possible role of the enzyme in morphological control and its potential as a chemotherapeutic target are discussed...
Synergism between 9-deazainosine and DL-alpha-difluoromethylornithine in treatment of experimental African trypanosomiasisC J Bacchi
Department of Biology, Pace University, New York, New York 10038
Antimicrob Agents Chemother 31:1406-13. 1987..These studies indicate that 9-DINO is a potent, nontoxic purine analog which, in combination with DFMO, is capable of late-stage cures of African trypanosomiasis...
Novel trypanocidal analogs of 5'-(methylthio)-adenosineJanice R Sufrin
Department of Pharmacology and Therapeutics, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
Antimicrob Agents Chemother 52:211-9. 2008..This suggests that additional biochemical mechanisms are associated with the trypanocidal effects of HETA and its analogs...
Synthesis and evaluation of analogues of 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine as inhibitors of tumor cell growth, trypanosomal growth, and HIV-1 infectivityCanio J Marasco
Department of Pharmacology and Therapeutics, Grace Cancer Drug Center, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
J Med Chem 45:5112-22. 2002..Moreover, the acetylated derivative of 5'-([(Z)-4-amino-2-butenyl]methylamino)-5'-deoxyadenosine did inhibit HIV-1 growth and infectivity, whereas the parent compound did not...
Identification and characterization of a novel flavin-containing spermine oxidase of mammalian cell originSlavoljub Vujcic
Grace Cancer Drug Center, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
Biochem J 367:665-75. 2002....
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activityXiangdong Bi
Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Ave, Detroit, MI 48202, USA
Bioorg Med Chem Lett 16:3229-32. 2006..The most effective analogues, 7a, 7b and 8d, inhibited parasitic growth in vitro with IC50 values of 0.18, 0.09 and 0.18 microM, respectively. These agents represent a promising new class of potential antitrypanosomal agents...
Trypanocidal activity of piperazine-linked bisbenzamidines and bisbenzamidoxime, an orally active prodrugTien L Huang
College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
Int J Antimicrob Agents 30:555-61. 2007..Three compounds (7, 11 and 15) provided 100% cure when administered parenterally. The results indicate that the nature of the substituents at the amidinium nitrogens of bisbenzamidines strongly influence their trypanocidal activity...
