Baylis-Hillman reaction assisted parallel synthesis of 3,5-disubstituted isoxazoles and their in vivo bioevaluation as antithrombotic agents

被引:45
作者
Batra, S [1 ]
Roy, AK
Patra, A
Bhaduri, AP
Surin, WR
Raghavan, SAV
Sharma, P
Kapoor, K
Dikshit, M
机构
[1] Cent Drug Res Inst, Div Med Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Pharmacol, Lucknow 226001, Uttar Pradesh, India
关键词
Baylis-Hillman reaction; isoxazolecarbaldehyde; isoxazole; nucleophilic substitution; substituted piperazine; antithrombotic activity; platelet aggregation;
D O I
10.1016/j.bmc.2004.02.023
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The solution-phase parallel synthesis involving reactions of Baylis-Hillman products of 3-substituted -5-isoxazolecarb-aldehydes with nucleophiles and their in vivo antithrombotic evaluations are described along with the results of in vitro platelet aggregation inhibition assay of a few compounds. Results of the detailed evaluation of one of the compounds as an inhibitor of platelet aggregation are also presented. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2059 / 2077
页数:19
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