Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines as potent analgesic and anti-inflammatory agents

被引：37

作者：

Chhabria, Mahesh T. ^{[1
]}

Bhatt, Hardik G.

Raval, Hitesh G.

Oza, Pratik M.

机构：

[1] LM Coll Pharm, Ahmadabad 380009, Gujarat, India

[2] NIRMA Univ Sci & Technol, Inst Pharm, Ahmadabad 382481, Gujarat, India

[3] Anand Pharm Coll, Anand 388001, Gujarat, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 04期

关键词：

aminopyrimidines; analgesic; anti-inflammatory; cyclooxygenase; NSAIDs;

D O I：

10.1016/j.bmcl.2006.11.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines have been achieved by cyclization of N-[2-ethoxycarbonyl-2-cyano-1-(isopropylamino)vinyl] formamidine in presence of dry HCl in dioxane followed by nucleophilic substitution of 4-chloro group with substituted aromatic amine or phenoxide. Target compounds were evaluated for their analgesic and anti-inflammatory potential by known experimental models. Some of the compounds emerged out as more potent than standard drugs. Very low ulcer index was observed for the potent compounds. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1022 / 1024

页数：3

共 10 条

[1] Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) as a new strategy to provide safer non-steroidal anti-inflammatory drugs [J].