mediabstractf2002 - American Chemical Society Division of...

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Unformatted text preview: American Chemical Society Division of Medicinal Chemistry ABSTRACTS 224th ACS National Meeting Boston, MA August 18-22, 2002 W. J. Greenlee, Program Chair SUNDAY MORNING General Oral Papers S. Chackalamannil, Presiding Papers 1-9 SUNDAY AFTERNOON General Oral Papers R. Wagner, Presiding Papers 10-18 Non-HIV Antivirals C. Tseng, Organizer, Presiding; W. J. Brouillette, Organizer Papers 19-24 SUNDAY EVENING Poster Session W. J. Greenlee, Organizer Papers 25-196 MONDAY MORNING Graduate Student Fellowship Award Symposium W. J. Greenlee, Organizer Papers 197-201 MONDAY AFTERNOON General Oral Papers W. J. Brouillette, Presiding Papers 202-210 Polyamine Based Therapeutics M. Burns, Organizer, Presiding; D. Bergstrom, Organizer Papers 211-215 MONDAY EVENING Sci-Mix A. B. Cooper, Presiding Papers 26-27, 29-30, 38, 44, 46, 48-49, 54-57, 61, 63, 65-66, 68, 72, 78, 82, 86-87, 97-99, 102-103, 108-114, 116, 118-119, 123, 127-128, 133-134, 138, 148-154, 156, 162-164, 166-167, 169-170, 172-179, 183, 186, 188-189, 193-194, 241-242, 246, 249-250, 253-256, 261, 265, 271, 278-284, 290, 296-297, 308, 310, 314-316, 318, 320, 322, 326, 331, 338-339, 343-347, 349, 359, 363, 366-367, 381-383, 386-388, 391-393, 399, 403, 405-406 TUESDAY MORNING General Oral Papers B. Wang, Presiding Papers 216-223 Histone Modifications C. A. Caperelli, Organizer Papers 224-227 TUESDAY AFTERNOON General Oral Papers P. Woster, Presiding Papers 228-235 WEDNESDAY MORNING Antitumor Natural Products F. R. ,. J. Kinder, Organizer Papers 236-240 Poster Session W. J. Greenlee, Organizer Papers 241-406 WEDNESDAY AFTERNOON General Oral Papers L. J. Lombardo, Presiding Papers 407-415 Adenosine Receptor Modulators K. A. Jacobson, Organizer Papers 416-421 THURSDAY MORNING Metalloproteinase Inhibitors L. W. McQuire, Organizer Papers 422-426 THURSDAY AFTERNOON Caspase Inhibitors D. Rotella, Organizer Papers 427-430 1. KEY ROLE OF DEVELOPABILITY CRITERIA IN THE DISCOVERY OF SB-435495: A POTENT, ORALLY ACTIVE INHIBITOR OF LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A 2 FOR EVALUATION IN MAN. Stephen A Smith, Medicines Research Centre, GlaxoSmithKline, Gunnels Wood Road, Stevenage, SG1 2NY, United Kingdom, Fax: 0044-1438-763620, stephen_1_smith@gsk.com Lipoprotein-associated phospholipase A 2 (Lp-PLA 2 ) has been suggested to play a key role in atherosclerotic plaque formation and development. Indeed Lp-PLA 2 has been shown to be a new, independent marker of coronary heart disease risk. Inhibition of this lipase then represents an exciting new therapeutic opportunity for the treatment of atherosclerosis. With this opportunity in mind, a weak HTS lead has been modified to give inhibitors ( 1 , X=Cl, CF 3 , Ar=1-Me- pyrazol-4-yl or 2-MeO-pyrimidin-5-yl) of nanomolar potency and good oral activity. This presentation will describe the optimisation of these inhibitors and in particular highlight the use of developability filters to accelerate the optimisa-...
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mediabstractf2002 - American Chemical Society Division of...

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