BALANCED ANGIOTENSIN-II RECEPTOR ANTAGONISTS .3. THE EFFECTS OF SUBSTITUTION AT THE IMIDAZOLE 5-POSITION

被引:18
作者
SANTELLA, JB [1 ]
DUNCIA, JV [1 ]
ENSINGER, CL [1 ]
VANATTEN, MK [1 ]
CARINI, DJ [1 ]
WEXLER, RR [1 ]
CHIU, AT [1 ]
WONG, PC [1 ]
TIMMERMANS, PBMWM [1 ]
机构
[1] DUPONT MERCK PHARMACEUT CO,EXPTL STN,WILMINGTON,DE 19880
关键词
D O I
10.1016/S0960-894X(00)80077-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We wish to report on a series of substituted methyl esters and amides of DMP 811, which bind to both the AT(1) and AT(2) receptor subtypes. Some of the esters bind well to both receptor subtypes in the subnanomolar range when the optimal acid isostere is present together with an ortho-fluorine substituent on the biphenylmethyl group.
引用
收藏
页码:2235 / 2240
页数:6
相关论文
共 16 条
[1]   SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A NOVEL SERIES OF NONPEPTIDE ANGIOTENSIN-II RECEPTOR-BINDING INHIBITORS SPECIFIC FOR THE AT2 SUBTYPE [J].
BLANKLEY, CJ ;
HODGES, JC ;
KLUTCHKO, SR ;
HIMMELSBACH, RJ ;
CHUCHOLOWSKI, A ;
CONNOLLY, CJ ;
NEERGAARD, SJ ;
VANNIEUWENHZE, MS ;
SEBASTIAN, A ;
QUIN, J ;
ESSENBURG, AD ;
COHEN, DM .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (11) :3248-3260
[2]   NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF DMP-581 AND DMP-811 [J].
CARINI, DJ ;
ARDECKY, RJ ;
ENSINGER, CL ;
PRUITT, JR ;
WEXLER, RR ;
WONG, PC ;
HUANG, SM ;
AUNGST, BJ ;
TIMMERMANS, PBMWM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) :63-68
[3]  
CHANG RSL, 1992, J PHARMACOL EXP THER, V262, P133
[4]  
Chiu A T, 1990, Receptor, V1, P33
[5]  
CHIU AT, 1990, J PHARMACOL EXP THER, V252, P711
[6]  
CHIU AT, 1993, CELLULAR MOL BIOL RE, P245
[7]   A POTENT, ORALLY-ACTIVE, BALANCED AFFINITY ANGIOTENSIN-II AT(1) ANTAGONIST AND AT(2) BINDING INHIBITOR [J].
DELASZLO, SE ;
QUAGLIATO, CS ;
GREENLEE, WJ ;
PATCHETT, AA ;
CHANG, RSL ;
LOTTI, VJ ;
CHEN, TB ;
SCHECK, SA ;
FAUST, KA ;
KIVLIGHN, SS ;
SCHORN, TS ;
ZINGARO, GJ ;
SIEGL, PKS .
JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (21) :3207-3210
[8]   THE DISCOVERY OF DUP-753, A POTENT, ORALLY ACTIVE NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST [J].
DUNCIA, JV ;
CARINI, DJ ;
CHIU, AT ;
JOHNSON, AL ;
PRICE, WA ;
WONG, PC ;
WEXLER, RR ;
TIMMERMANS, PBMWM .
MEDICINAL RESEARCH REVIEWS, 1992, 12 (02) :149-191
[9]   A NEW CLASS OF BALANCED AT(1)/AT(2) ANGIOTENSIN-II ANTAGONISTS - QUINAZOLINONE AII ANTAGONISTS WITH ACYLSULFONAMIDE AND SULFONYLCARBAMATE ACIDIC FUNCTIONALITIES [J].
GLINKA, TW ;
DELASZLO, SE ;
SIEGL, PKS ;
CHANG, RS ;
KIVLIGHN, SD ;
SCHORN, TS ;
FAUST, KA ;
CHEN, TB ;
ZINGARO, GJ ;
LOTTI, VJ ;
GREENLEE, WJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) :81-86
[10]  
Lo Y. S., 1992, Patent No. [US5130439, 5130439]