A NEW CLASS OF LEUKOTRIENE BIOSYNTHESIS INHIBITORS - THE DISCOVERY OF MK0591

被引：10

作者：

PRASIT, P

BELLEY, M

BRIDEAU, C

CHAN, C

CHARLESON, S

EVANS, JF

FORTIN, R

FORDHUTCHINSON, AW

GILLARD, JW

GUAY, J

HUTCHINSON, JH

LEGER, S

RIENDEAU, D

YOUNG, RN

ZAMBONI, R

机构：

[1] Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Que. H9R 4P8

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(00)80520-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The evolution of a quinoline based FLAP inhibitor, L-674,636, into a novel quinoline-indole hybrid compound: MK0591, is described. The new series of compounds are more potent, particularly in binding to FLAP, in inhibiting LTB4 biosynthesis in stimulated human PMN, and in the human whole blood assay.

引用

页码：1395 / 1398

页数：4

共 9 条

[1] BRIDEAU C, 1992, IN PRESS CAN J PHYSL
[2] CHARLESON S, 1992, MOL PHARMACOL, V41, P873
[3] REQUIREMENT OF A 5-LIPOXYGENASE-ACTIVATING PROTEIN FOR LEUKOTRIENE SYNTHESIS
DIXON, RAF
DIEHL, RE
OPAS, E
RANDS, E
VICKERS, PJ
EVANS, JF
GILLARD, JW
MILLER, DK
[J]. NATURE, 1990, 343 (6255) : 282 - 284
[4] EVANS JF, 1991, MOL PHARMACOL, V40, P22
[5] L-663,536 (MK-886) (3-[1-(4-CHLOROBENZYL)-3-T-BUTYL-THIO-5-ISOPROPYLINDOL-2-YL]-2,2-DIMETHYLPROPANOIC ACID), A NOVEL, ORALLY ACTIVE LEUKOTRIENE BIOSYNTHESIS INHIBITOR
GILLARD, J
FORDHUTCHINSON, AW
CHAN, C
CHARLESON, S
DENIS, D
FOSTER, A
FORTIN, R
LEGER, S
MCFARLANE, CS
MORTON, H
PIECHUTA, H
RIENDEAU, D
ROUZER, CA
ROKACH, J
YOUNG, R
MACINTYRE, DE
PETERSON, L
BACH, T
EIERMANN, G
HOPPLE, S
HUMES, J
HUPE, L
LUELL, S
METZGER, J
MEURER, R
MILLER, DK
OPAS, E
PACHOLOK, S
[J]. CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY, 1989, 67 (05) : 456 - 464
[6] IDENTIFICATION AND ISOLATION OF A MEMBRANE-PROTEIN NECESSARY FOR LEUKOTRIENE PRODUCTION
MILLER, DK
GILLARD, JW
VICKERS, PJ
SADOWSKI, S
LEVEILLE, C
MANCINI, JA
CHARLESON, P
DIXON, RAF
FORDHUTCHINSON, AW
FORTIN, R
GAUTHIER, JY
RODKEY, J
ROSEN, R
ROUZER, C
SIGAL, IS
STRADER, CD
EVANS, JF
[J]. NATURE, 1990, 343 (6255) : 278 - 281
[7] PRASIT P, 1991, BIOMED CHEM LETT, P645
[8] ROUZER CA, 1990, J BIOL CHEM, V265, P1436
[9] ROUZER CA, 1988, J BIOL CHEM, V263, P1436

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