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

被引：61

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
Andersson, KE
[J]. UROLOGY, 1997, 50 (6A) : 74 - 84
[2] Pharmacological and molecular analysis of ATP-sensitive K+ channels in the pig and human detrusor
Buckner, SA
Milicic, I
Daza, A
Davis-Taber, R
Scott, VES
Sullivan, JP
Brioni, JD
[J]. 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
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
[J]. 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
Coghlan, MJ
Carroll, WA
Gopalakrishnan, M
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (11) : 1627 - 1653
[7] DIHYDROPYRIDINE KATP POTASSIUM CHANNEL OPENERS
FRANK, CA
FORST, JM
GRANT, T
HARRIS, RJ
KAU, ST
LI, JH
OHNMACHT, CJ
SMITH, RW
TRAINOR, DA
TRIVEDI, S
[J]. 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
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
[J]. 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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