The discovery of novel, potent and selective PDE5 inhibitors

被引：21

作者：

Bi, YZ

Stoy, P

Adam, L

He, B

Krupinski, J

Normandin, D

Pongrac, R

Seliger, L

Watson, A

Macor, JE

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Metab & Cardiovasc Drug Discovery, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(01)00466-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and synthesis of a novel scaffold for potent and selective PDE5 inhibitors are described. Compound 3a was more potent (PDE5 IC50 = 0.31 nM) and selective (> 10,000-fold vs PDE1 and 160-fold selective vs PDE6) PDE5 inhibitor than sildenafil. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2461 / 2464

页数：4

共 13 条

[1] PHYSIOLOGY OF PENILE ERECTION
ANDERSSON, KE
WAGNER, G
[J]. PHYSIOLOGICAL REVIEWS, 1995, 75 (01) : 191 - 236
[2] CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES - FUNCTIONAL IMPLICATIONS OF MULTIPLE ISOFORMS
BEAVO, JA
[J]. PHYSIOLOGICAL REVIEWS, 1995, 75 (04) : 725 - 748
[3] BI Y, UNPUB
[4] Boolell M, 1996, Int J Impot Res, V8, P47
[5] Eardley I, 1997, Expert Opin Investig Drugs, V6, P1803, DOI 10.1517/13543784.6.12.1803
[6] Drugs for the treatment of impotence
GarciaReboll, L
Mulhall, JP
Goldstein, I
[J]. DRUGS & AGING, 1997, 11 (02) : 140 - 151
[7] Phosphodiesterase 5 inhibitors and nitrergic transmission - from zaprinast to sildenafil
Gibson, A
[J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 2001, 411 (1-2) : 1 - 10
[8] Martel A. M., 1997, Drugs of the Future, V22, P138
[9] N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction
Rotella, DP
Sun, Z
Zhu, YH
Krupinski, J
Pongrac, R
Seliger, L
Normandin, D
Macor, JE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (07) : 1257 - 1263
[10] A CONVENIENT SYNTHESIS OF PYRAZOLO[3,4-B]PYRIDINE NUCLEOSIDES BY CONVENIENT RING-CLOSURE PROCEDURES - X-RAY CRYSTAL AND MOLECULAR-STRUCTURE OF 4-AMINO-1-(BETA-D-RIBOFURANOSYL)-1,7-DIHYDROPYRAZOLO[3,4-B]PYRIDIN-6-ONE
SANGHVI, YS
LARSON, SB
ROBINS, RK
REVANKAR, GR
[J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1990, (11): : 2943 - 2950

← 1 2 →