Youssef L Bennani

Summary

Affiliation: Pharmaceutical Products Division
Country: USA

Publications

  1. ncbi request reprint Identification of novel and improved antimitotic agents derived from noscapine
    James T Anderson
    Athersys, Inc, 3201 Carnegie Avenue, Cleveland, Ohio 44115 2634, USA
    J Med Chem 48:7096-8. 2005
  2. ncbi request reprint Aza-retinoids as novel retinoid X receptor-specific agonists
    Luc J Farmer
    Ligand Pharmaceuticals Inc, 10255 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:2352-6. 2006
  3. ncbi request reprint Discovery, SAR, synthesis, pharmacokinetic and biochemical characterization of A-192411: a novel fungicidal lipopeptide-(I)
    Weibo Wang
    Infectious Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 13:489-93. 2003
  4. ncbi request reprint In vivo characterization of A-192411: a novel fungicidal lipopeptide (II)
    Jonathan A Meulbroek
    Infectious Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 13:495-7. 2003
  5. ncbi request reprint 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention
    Marlon Cowart
    Department of Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 48:38-55. 2005
  6. ncbi request reprint Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties
    Timothy A Esbenshade
    Neuroscience Research, Abbott Laboratories, R4MN, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    J Pharmacol Exp Ther 313:165-75. 2005
  7. ncbi request reprint Evidence for tolerance following repeated dosing in rats with ciproxifan, but not with A-304121
    Jia Bao Pan
    Neuroscience Research, Abbott Laboratories, 100 Abbott Road, Abbott Park, IL 60064 6125, USA
    Life Sci 79:1366-79. 2006
  8. ncbi request reprint 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration
    Lawrence A Black
    Neuroscience Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 17:1443-6. 2007
  9. ncbi request reprint Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist
    Timothy A Esbenshade
    Abbott Laboratories, Global Pharmaceutical Research Division, Department of Neuroscience Research, Abbott Park, IL 60064, USA
    Biochem Pharmacol 68:933-45. 2004
  10. ncbi request reprint Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 re
    Gerard B Fox
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, AP9A, R4N5, Abbott Park, IL 60064 6115, USA
    J Pharmacol Exp Ther 313:176-90. 2005

Collaborators

Detail Information

Publications30

  1. ncbi request reprint Identification of novel and improved antimitotic agents derived from noscapine
    James T Anderson
    Athersys, Inc, 3201 Carnegie Avenue, Cleveland, Ohio 44115 2634, USA
    J Med Chem 48:7096-8. 2005
    ..1 microM and also affects tubulin polymerization. Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells...
  2. ncbi request reprint Aza-retinoids as novel retinoid X receptor-specific agonists
    Luc J Farmer
    Ligand Pharmaceuticals Inc, 10255 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:2352-6. 2006
    ..Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series...
  3. ncbi request reprint Discovery, SAR, synthesis, pharmacokinetic and biochemical characterization of A-192411: a novel fungicidal lipopeptide-(I)
    Weibo Wang
    Infectious Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 13:489-93. 2003
    ..Namely A-192411 shows good in vitro activity against common pathogenic yeasts and has an acceptable safety window in vivo. Discovery, limited SAR, synthesis, biochemical and pharmaco-dynamic profiles of A-192411 are presented...
  4. ncbi request reprint In vivo characterization of A-192411: a novel fungicidal lipopeptide (II)
    Jonathan A Meulbroek
    Infectious Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 13:495-7. 2003
    ..A-192411 also slightly prolonged the survival of immunocompromised mice infected systemically with Aspergillus fumigatus...
  5. ncbi request reprint 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention
    Marlon Cowart
    Department of Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 48:38-55. 2005
    ..The potency and selectivity of this compound and of analogues from this class support the potential of H(3) receptor antagonists for the treatment of cognitive dysfunction...
  6. ncbi request reprint Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties
    Timothy A Esbenshade
    Neuroscience Research, Abbott Laboratories, R4MN, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    J Pharmacol Exp Ther 313:165-75. 2005
    ..Thus, ABT-239 is a selective, nonimidazole H3 receptor antagonist/inverse agonist with similar high potency in both human and rat and favorable drug-like properties...
  7. ncbi request reprint Evidence for tolerance following repeated dosing in rats with ciproxifan, but not with A-304121
    Jia Bao Pan
    Neuroscience Research, Abbott Laboratories, 100 Abbott Road, Abbott Park, IL 60064 6125, USA
    Life Sci 79:1366-79. 2006
    ..The implications for potential long-term treatment with H(3) receptor antagonists in CNS disorders such as ADHD are discussed...
  8. ncbi request reprint 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration
    Lawrence A Black
    Neuroscience Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 17:1443-6. 2007
    ..The SAR of the tertiary amine moiety is similar to that reported for the benzofuran series, with analogs bearing a 2-methylpyrrolidine substituent possessing the greatest rat and human H3 receptor binding affinities...
  9. ncbi request reprint Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist
    Timothy A Esbenshade
    Abbott Laboratories, Global Pharmaceutical Research Division, Department of Neuroscience Research, Abbott Park, IL 60064, USA
    Biochem Pharmacol 68:933-45. 2004
    ..Thus, A-349821 is a novel, selective non-imidazole H3 antagonist/inverse agonist with balanced high potency across species and favorable cognition enhancing effects in rats...
  10. ncbi request reprint Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 re
    Gerard B Fox
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, AP9A, R4N5, Abbott Park, IL 60064 6115, USA
    J Pharmacol Exp Ther 313:176-90. 2005
    ..0 mg/kg), but not striatum. In summary, broad efficacy was observed with ABT-239 across animal models such that potential clinical efficacy may extend beyond disorders such as ADHD to include Alzheimer's disease and schizophrenia...
  11. doi request reprint Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships
    Chen Zhao
    Department of Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 52:4640-9. 2009
    ..54 nM, rat H3 K(i) of 4.57 nM, and excellent pharmacokinetics (PK) profile in rats (oral bioavailability of 39% and t(1/2) of 2.4 h)...
  12. ncbi request reprint D-amino acid homopiperazine amides: discovery of A-320436, a potent and selective non-imidazole histamine H(3)-receptor antagonist
    Michael P Curtis
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Arch Pharm (Weinheim) 337:219-29. 2004
    ..This compound was shown to demonstrate in vitro and in vivo functional antagonism and is non-neurotoxic at doses (i.p.) up to 163 mg/kg in a general observation test...
  13. doi request reprint The alkaloid conessine and analogues as potent histamine H3 receptor antagonists
    Chen Zhao
    Department of Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 51:5423-30. 2008
    ..One optimized analogue (13c) was examined in detail and was found to be efficacious in animal behavioral model of cognition...
  14. ncbi request reprint Structure-activity relationships of arylbenzofuran H3 receptor antagonists
    Gregory A Gfesser
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 15:2559-63. 2005
    ..An SAR study of histamine H3 receptor antagonists based on substituted (R)-2-methyl-1-[2-(5-phenyl-benzofuran-2-yl)-ethyl]-pyrrolidines is presented...
  15. ncbi request reprint Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist
    Arthur A Hancock
    Abbott Laboratories, Global Pharmaceutical Research and Development, 100 Abbott Park Road, Abbott Park, IL 60064 6125, USA
    Eur J Pharmacol 487:183-97. 2004
    ..The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent...
  16. ncbi request reprint A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans
    Marlon Cowart
    Department of Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    Bioorg Med Chem Lett 14:689-93. 2004
    ..The SAR of the basic amine moiety was compared in three different series of analogues. The greatest potency was found in analogues bearing a 2-methylpyrrolidine, a 2,5-dimethylpyrrolidine, or a 2,6-dimethylpiperidine...
  17. ncbi request reprint A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines
    Sean C Turner
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, 60064, Abbott Park, IL, USA
    Bioorg Med Chem Lett 13:2131-5. 2003
    ..Modifications of the amino substituents, optimization of chain length and the effect of conformational restraints are described. Several compounds with high affinity and selectivity for the H(3) receptor were discovered...
  18. ncbi request reprint Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists
    Gregory A Gfesser
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 14:673-6. 2004
    ..Compound 14bb is a potent antagonist of both the rat cortical and human clone receptors, and is demonstrated to act functionally as an antagonist in an in vivo mouse dipsogenia model...
  19. ncbi request reprint Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists
    Michael J Robarge
    Athersys, Inc, Medicinal Chemistry, 3201 Carnegie Avenue, Cleveland, OH 44115 2634, USA
    Bioorg Med Chem Lett 15:1749-53. 2005
    ..In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases...
  20. ncbi request reprint The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors
    L Nathan Tumey
    Athersys, Inc, 3201 Carnegie Ave, Cleveland, OH 44115, USA
    Bioorg Med Chem Lett 15:277-81. 2005
    ..To our knowledge, these are the most potent endonuclease inhibitors reported to date...
  21. ncbi request reprint The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors
    L Nathan Tumey
    Athersys, Inc, 3201 Carnegie Ave, Cleveland, OH 44115, USA
    Bioorg Med Chem Lett 14:4915-8. 2004
    ..In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors...
  22. ncbi request reprint An efficient multigram synthesis of the potent histamine H3 antagonist GT-2331 and the reassessment of the absolute configuration
    Huaqing Liu
    Neuroscience Research, Global Pharmaceutical Research Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6123, USA
    J Org Chem 69:192-4. 2004
    ..However, we found that the dextrorotatory, more potent, enantiomer of 4-[2-(5,5-dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole has the (1S,2S) absolute configuration. We suggest a reconsideration of the absolute configuration of GT-2331...
  23. ncbi request reprint Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park 60064 6123, USA
    Bioorg Med Chem Lett 13:1325-8. 2003
    ..Most compounds were highly potent and selective for human and rat H(3) receptors and selected examples such as A-349821 showed functional antagonism of H(3) receptors in vitro and in a mouse dipsogenia model...
  24. ncbi request reprint Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    Bioorg Med Chem Lett 12:2031-4. 2002
    ..A high throughput screening lead, A-923, was further elaborated in a systematic manner to clarify a pharmacophore for this class of aryloxyalkyl piperazine based compounds...
  25. ncbi request reprint Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    Bioorg Med Chem Lett 12:3077-9. 2002
    ..Biaryl nitrile amines were prepared and found to have high affinity and selectivity for human and rat histamine H(3) receptors...
  26. ncbi request reprint Synthesis and evaluation of potent pyrrolidine H(3) antagonists
    Anil Vasudevan
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60031, USA
    Bioorg Med Chem Lett 12:3055-8. 2002
    ..A systematic modification of the substituents on the aminopyrrolidine ring was performed using pre-formatted precursor sets, where applicable, to afford several compounds with high affinity and selectivity for the H(3) receptor...
  27. ncbi request reprint Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs
    Ramin Faghih
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    Bioorg Med Chem Lett 12:2035-7. 2002
    ..Structure-activity relationship studies on novel non-imidazole, D-amino acid containing ligands of histamine 3 receptors are presented. A-304121 is a D-alanine piperazine amide with high affinity at the rat H(3) receptor...
  28. ncbi request reprint Discovery of S-phase arresting agents derived from noscapine
    James T Anderson
    Athersys, Inc, 3201 Carnegie Avenue, Cleveland, Ohio 44115 2634, USA
    J Med Chem 48:2756-8. 2005
    ..Compound 4a was the most potent analogue inhibiting cell proliferation at an EC(50) of 1.9 microM...
  29. ncbi request reprint The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist
    Bayard R Huck
    Athersys, Inc, 3201 Carnegie Ave, Cleveland, OH 44115, USA
    Bioorg Med Chem Lett 16:4130-4. 2006
    ..The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats...
  30. ncbi request reprint The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists
    Bayard R Huck
    Athersys, Inc, 3201 Carnegie Ave, Cleveland, OH 44115, USA
    Bioorg Med Chem Lett 16:2891-4. 2006
    ..3.0]octane series. This compound displayed good potency at the 5-HT2C receptor, modest selectivity relative to other 5-HT2 receptors, and was efficacious in an acute feeding study in rats...