Synthesis, anticoagulant and PIVKA-II induced by new 4-hydroxycoumarin derivatives

被引：126
|
作者：
Abdelhafez, Omaima M. [1 ]
Amin, Kamelia M. [2 ]
Batran, Rasha Z. [1 ]
Maher, Timothy J. [3 ]
Nada, Somaia A. [4 ]
Sethumadhavan, Shalini [3 ]
机构：
[1] Natl Res Ctr, Dept Chem Nat Prod, Cairo, Egypt
[2] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt
[3] Boston Univ, Massachusettes Coll Pharm & Hlth Sci, Boston, MA 02215 USA
[4] Natl Res Ctr, Dept Pharmacol, Cairo, Egypt
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 10期
关键词：
4-Hydroxycoumarin; Pyridines; Pyrimidines; Pyrazoles; Anticoagulant; PIVKA-II; VITAMIN-K; HIGHLY POTENT; DISCOVERY; WARFARIN; PLASMA; REDUCTASE;
D O I：
10.1016/j.bmc.2010.04.009
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 action of the coumarin-type drugs and related compounds is reviewed to their VKOR antagonistic effects. In our study, twenty 3-pyridinyl, pyrimidinyl and pyrazolyl-4-hydroxycoumarin derivatives were synthesized. A comparative in vivo (CT, PT determination) and in vitro ( measurement of PIVKA-II levels) anticoagulant study with respect to warfarin showed that the synthesized compounds have different anticoagulant activities, the most prospective compounds were the 3-pyrazolyl-4-hydroxycoumarin derivatives. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3371 / 3378
页数：8
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