BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .3. POTENT AND ORALLY-ACTIVE 5-BETA-KETOSULFOXIDE IMIDAZOLYL BIPHENYL SULFONYLUREAS

被引：6

作者：

DEPREZ, P

GUILLAUME, J

CORBIER, A

VEVERT, JP

FORTIN, M

HECKMANN, B

机构：

[1] Roussel Uclaf, 93235 Romainville Cedex

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00480-H

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the imidazolyl biphenyl sulfonylurea series, effects of substitution in position 5 of the imidazole ring with enolic ketone moiety were studied on AT(2) binding. beta-ketosulfoxide, beta-ketosulfone and beta-ketoester proved to be highly effective substituents for potent nanomolar binding affinity on both AT(1) and AT(2) receptor subtypes. This led to the identification of beta-ketophenylsulfoxide RU 64276 as a potent and orally active AT(1) antagonist and AT(2) binding inhibitor.

引用

页码：2617 / 2622

页数：6

共 20 条

[1] ASHTON WT, 1994, EXPERT OPIN INV DRUG, V3, P1105
[2] BUHLMAYER P, 1992, CURR OPIN THER PAT, V2, P1693
[3] NOMENCLATURE FOR ANGIOTENSIN RECEPTORS - A REPORT OF THE NOMENCLATURE-COMMITTEE OF THE COUNCIL-FOR-HIGH-BLOOD-PRESSURE-RESEARCH
BUMPUS, FM
CATT, KJ
CHIU, AT
DEGASPARO, M
GOODFRIEND, T
HUSAIN, A
PEACH, MJ
TAYLOR, DG
TIMMERMANS, PBMWM
[J]. HYPERTENSION, 1991, 17 (05) : 720 - 721
[4] TRIAZOLINONE BIPHENYLSULFONAMIDES AS ANGIOTENSIN-II RECEPTOR ANTAGONISTS WITH HIGH-AFFINITY FOR BOTH THE AT(1) AND AT(2) SUBTYPES
CHANG, LL
ASHTON, WT
FLANAGAN, KL
CHEN, TB
OMALLEY, SS
ZINGARO, GJ
SIEGL, PKS
KIVLIGHN, SD
LOTTI, VJ
CHANG, RSL
GREENLEE, WJ
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (26) : 4464 - 4478
[5] ORAL-ADMINISTRATION OF DUP-753, A SPECIFIC ANGIOTENSIN-II RECEPTOR ANTAGONIST, TO NORMAL-MALE VOLUNTEERS - INHIBITION OF PRESSOR-RESPONSE TO EXOGENOUS ANGIOTENSIN-I AND ANGIOTENSIN-II
CHRISTEN, Y
WAEBER, B
NUSSBERGER, J
PORCHET, M
BORLAND, RM
LEE, RJ
MAGGON, K
SHUM, L
TIMMERMANS, PBMWM
BRUNNER, HR
[J]. CIRCULATION, 1991, 83 (04) : 1333 - 1342
[6] CORVOL P, 1989, CLIN EXP HYPERTENS A, V11, P463
[7] SULFONYLUREAS AND SULFONYLCARBAMATES AS NEW NON-TETRAZOLE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - DISCOVERY OF A HIGHLY POTENT ORALLY-ACTIVE (IMIDAZOLYLBIPHENYLYL) SULFONYLUREA (HR-720)
DEPREZ, P
GUILLAUME, J
BECKER, R
CORBIER, A
DIDIERLAURENT, S
FORTIN, M
FRECHET, D
HAMON, G
HECKMANN, B
HEITSCH, H
KLEEMANN, HW
VEVERT, JP
VINCENT, JC
WAGNER, A
ZHANG, JD
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (13) : 2357 - 2377
[8] DEPREZ P, IN PRESS BIOORG ME 1
[9] DEPREZ P, IN PRESS BIOORG ME 2
[10] THE RENIN-ANGIOTENSIN SYSTEM - IMPORTANCE IN PHYSIOLOGY AND PATHOLOGY
FERRARIO, CM
[J]. JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1990, 15 : S1 - S5

← 1 2 →