Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets

被引：14

作者：

Yamada, Y ^{[1
]}

Ando, K ^{[1
]}

Komiyama, K ^{[1
]}

Shibata, S ^{[1
]}

Nakamura, I ^{[1
]}

Hayashi, Y ^{[1
]}

Ikegami, K ^{[1
]}

Uchida, I ^{[1
]}

机构：

[1] YOSHITOMI PHARMACEUT IND LTD,RES LABS,IRUMA,SAITAMA 358,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(97)00323-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of low molecular renin inhibitors (molecular weight < 600) were prepared and their biological activities were evaluated. The inhibitors containing indole-2-carbonyl moieties at the P3 position and 2-amino-3,5-anti-diol fragment at the Pl-Pl' position showed renin inhibitory activities with IC50 of 10 (-8) M order and good blood pressure lowering effects after oral administration to sodium-depleted marmosets, (C) 1997 Elsevier Science Ltd.

引用

页码：1863 / 1868

页数：6

共 8 条

[1] NONPEPTIDE RENIN INHIBITORS WITH GOOD INTRADUODENAL BIOAVAILABILITY AND EFFICACY IN DOG [J].

BOYD, SA ;

FUNG, AKL ;

BAKER, WR ;

MANTEI, RA ;

STEIN, HH ;

COHEN, J ;

BARLOW, JL ;

KLINGHOFER, V ;

WESSALE, JL ;

VERBURG, KM ;

POLAKOWSKI, JS ;

ADLER, AL ;

CALZADILLA, SV ;

KOVAR, P ;

YAO, ZL ;

HUTCHINS, CW ;

DENISSEN, JF ;

GRABOWSKI, BA ;

CEPA, S ;

HOFFMAN, DJ ;

GARREN, KW ;

KLEINERT, HD .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (19) :2991-3007

[2] (PHOSPHINYLOXY)ACYL AMINO-ACID INHIBITORS OF ANGIOTENSIN CONVERTING ENZYME .2. TERMINAL AMINO-ACID-ANALOGS OF (S)-1-[6-AMINO-2-[[HYDROXY(4-PHENYLBUTYL)PHOSPHINYL]OXY]-1-OXOHEXYL]-L-PROLINE [J].

KARANEWSKY, DS ;

BADIA, MC ;

CUSHMAN, DW ;

DEFORREST, JM ;

DEJNEKA, T ;

LEE, VG ;

LOOTS, MJ ;

PETRILLO, EW .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1459-1469

[3] SYNTHESIS OF RIGID, HETEROCYCLIC DIPEPTIDE ANALOGS [J].

KEMPF, DJ ;

CONDON, SL .

JOURNAL OF ORGANIC CHEMISTRY, 1990, 55 (04) :1390-1394

[4] SYNTHESIS OF NOVEL ANGIOTENSIN CONVERTING-ENZYME-INHIBITOR QUINAPRIL AND RELATED-COMPOUNDS - A DIVERGENCE OF STRUCTURE-ACTIVITY-RELATIONSHIPS FOR NON-SULFHYDRYL AND SULFHYDRYL TYPES [J].

KLUTCHKO, S ;

BLANKLEY, CJ ;

FLEMING, RW ;

HINKLEY, JM ;

WERNER, AE ;

NORDIN, I ;

HOLMES, A ;

HOEFLE, ML ;

COHEN, DM ;

ESSENBURG, AD ;

KAPLAN, HR .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (10) :1953-1961

[5]

OCAIN T D, 1991, Drugs of the Future, V16, P37

[6]

SHIBATA S, 1991, 111 ANN M PHARM SOC, P90

[7]

SHIBATA S, 1991, 111 ANN M PHRM SOC J, P201

[8]

YAMADA Y, UNPUB CHEM PHARM B

← 1 →