STRUCTURE-ACTIVITY-RELATIONSHIPS OF 6-SUBSTITUTED BENZOPYRAN-4-CARBOTHIOAMIDE POTASSIUM CHANNEL OPENERS

被引：13

作者：

ISHIZAWA, T ^{[1
]}

KOGA, H ^{[1
]}

OHTA, M ^{[1
]}

SATO, H ^{[1
]}

MAKINO, T ^{[1
]}

KUROMARU, K ^{[1
]}

TAKA, N ^{[1
]}

TAKAHASHI, T ^{[1
]}

SATO, T ^{[1
]}

NABATA, H ^{[1
]}

机构：

[1] CHUGAI PHARMACEUT CO LTD, FUJI GOTEMBA RES LABS, 135 1 CHOME KOMAKADO, GOTEMBA, SHIZUOKA 412, JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80037-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

QSAR study of 6-substituted benzopyran-4-carbothioamides 1 showed that vasorelaxant activity is linearly correlated with the electronic parameter (sigmam) and parabolically correlated with steric (L) and hydrophobic (pi) parameters of the 6-substituent.

引用

页码：1659 / 1662

页数：4

共 13 条

[1] RELAXANT ACTIVITY OF 6-CYANO-2,2-DIMETHYL-2H-1-BENZOPYRAN-4-CARBOXAMIDES AND THIOCARBOXAMIDES AND THEIR ANALOGS IN GUINEA-PIG TRACHEALIS [J].

ARCH, JRS ;

BUCKLE, DR ;

CAREY, C ;

PARRDOBRZANSKI, H ;

FALLER, A ;

FOSTER, KA ;

HOUGEFRYDRYCH, CSV ;

PINTO, IL ;

SMITH, DG ;

TAYLOR, SG .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2588-2594

[2] SYNTHESIS AND ANTIHYPERTENSIVE ACTIVITY OF 4-(CYCLIC AMIDO)-2H-1-BENZOPYRANS [J].

ASHWOOD, VA ;

BUCKINGHAM, RE ;

CASSIDY, F ;

EVANS, JM ;

FARUK, EA ;

HAMILTON, TC ;

NASH, DJ ;

STEMP, G ;

WILLCOCKS, K .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (11) :2194-2201

[3] THE DESIGN OF A NOVEL CLASS OF POTASSIUM CHANNEL ACTIVATING DRUGS, 2-(2,2-DIMETHYLBENZOPYRAN-4-YL)-PYRIDINE-1-OXIDES [J].

ATTWOOD, MR ;

JONES, PS ;

KAY, PB ;

PACIOREK, PM ;

REDSHAW, S .

LIFE SCIENCES, 1991, 48 (08) :803-810

[4]

BRAY KM, 1992, J BIOL CHEM, V267, P11689

[5] CROSS-VALIDATION, BOOTSTRAPPING, AND PARTIAL LEAST-SQUARES COMPARED WITH MULTIPLE-REGRESSION IN CONVENTIONAL QSAR STUDIES [J].

CRAMER, RD ;

BUNCE, JD ;

PATTERSON, DE ;

FRANK, IE .

QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS, 1988, 7 (01) :18-25

[6] STRUCTURE-ACTIVITY-RELATIONSHIPS OF K+ CHANNEL OPENERS [J].

EDWARDS, G ;

WESTON, AH .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (10) :417-422

[7]

EVANS JM, 1991, ANNU REP MED CHEM, V26, P73

[8]

Hansch C. S., 1990, COMPREHENSIVE MED CH, V4

[9]

IMAGAWA J, UNPUB

[10] DESIGN OF POTENT K+ CHANNEL OPENERS BY PHARMACOPHORE MODEL [J].

KOGA, H ;

OHTA, M ;

SATO, H ;

ISHIZAWA, T ;

NABATA, H .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :625-631

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