Structure-activity studies for a novel series of tricyclic dihydropyrimidines as KATP channel openers (KCOs)

被引：62

作者：

Drizin, I ^{[1
]}

Holladay, MW ^{[1
]}

Yi, L ^{[1
]}

Zhang, HQ ^{[1
]}

Gopalakrishnan, S ^{[1
]}

Gopalakrishnan, M ^{[1
]}

Whiteaker, KL ^{[1
]}

Buckner, SA ^{[1
]}

Sullivan, JP ^{[1
]}

Carroll, WA ^{[1
]}

机构：

[1] Abbott Labs, GPRD, Neurosci, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(02)00207-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of tricyclic dihydropyrimidines was synthesized and evaluated for activity as K-ATP channel openers. The functional activity of several compounds, for example 6A (EC50 = 30 nM) and its enantiomers exceeded cromakalim. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1481 / 1484

页数：4

共 12 条

[1] The overactive bladder: Pharmacologic basis of drug treatment [J].

Andersson, KE .

UROLOGY, 1997, 50 (6A) :74-84

[2] Pharmacological and molecular analysis of ATP-sensitive K+ channels in the pig and human detrusor [J].

Buckner, SA ;

Milicic, I ;

Daza, A ;

Davis-Taber, R ;

Scott, VES ;

Sullivan, JP ;

Brioni, JD .

EUROPEAN JOURNAL OF PHARMACOLOGY, 2000, 400 (2-3) :287-295

[3] Design and SAR of novel potassium channel openers targeted for urge urinary incontinence.: 1.: N-cyanoguanidine bioisosteres possessing in vivo bladder selectivity [J].

Butera, JA ;

Antane, MM ;

Antane, SA ;

Argentieri, TM ;

Freeden, C ;

Graceffa, RF ;

Hirth, BH ;

Jenkins, D ;

Lennox, JR ;

Matelan, E ;

Norton, NW ;

Quagliato, D ;

Sheldon, JH ;

Spinelli, W ;

Warga, D ;

Wojdan, A ;

Woods, M .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (06) :1187-1202

[4]

CARROLL WA, 2001, Patent No. 6191140

[5]

Chess-Williams R, 1999, BJU INT, V83, P1050

[6] Recent developments in the biology and medicinal chemistry of potassium channel modulators: Update from a decade of progress [J].

Coghlan, MJ ;

Carroll, WA ;

Gopalakrishnan, M .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (11) :1627-1653

[7] DIHYDROPYRIDINE KATP POTASSIUM CHANNEL OPENERS [J].

FRANK, CA ;

FORST, JM ;

GRANT, T ;

HARRIS, RJ ;

KAU, ST ;

LI, JH ;

OHNMACHT, CJ ;

SMITH, RW ;

TRAINOR, DA ;

TRIVEDI, S .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (12) :2725-2726

[8] Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones [J].

Gilbert, AM ;

Antane, MM ;

Argentieri, TM ;

Butera, JA ;

Francisco, GD ;

Freeden, C ;

Gundersen, EC ;

Graceffa, RF ;

Herbst, D ;

Hirth, BH ;

Lennox, JR ;

McFarlane, G ;

Norton, NW ;

Quagliato, D ;

Sheldon, JH ;

Warga, D ;

Wojdan, A ;

Woods, M .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (06) :1203-1214

[9]

Gopalakrishnan M, 1999, J PHARMACOL EXP THER, V289, P551

[10]

Li JH, 1997, CARDIOVASC DRUG REV, V15, P220

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