Antimalarial activity of 2,4,6-trisubstituted pyrimidines

被引：36
作者：
Agarwal, A
Srivastava, K
Puri, SK
Chauhan, PMS [1 ]
机构：
[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 07期
关键词：
dihydrofolate reductase; antimalarial; pyrimidine;
D O I：
10.1016/j.bmcl.2005.02.015
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2,4,6-trisubstituted pyrimidines (3a-o) was synthesized and evaluated for their in vitro antimalarial activity against P. falciparum. Out of the 15 compounds synthesized 11 compounds showed MIC in the range of 0.5-2 mu g/mL. These compounds are in vitro several folds more active than pyrimethamine. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1881 / 1883
页数：3
相关论文
共 21 条
[1]   Syntheses of 2,4,6-trisubstituted triazines as antimalarial agents [J].
Agarwal, A ;
Srivastava, K ;
Puri, SK ;
Chauhan, PMS .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (03) :531-533
[2]   EXPERIMENTS ON THE SYNTHESIS OF PURINE NUCLEOSIDES .26. 9-D-GLUCOPYRANOSIDOISOGUANINE [J].
ANDREWS, KJM ;
ANAND, N ;
TODD, AR ;
TOPHAM, A .
JOURNAL OF THE CHEMICAL SOCIETY, 1949, (OCT) :2490-2497
[3]   Present trends and future strategy in chemotherapy of malaria [J].
Chauhan, PMS ;
Srivastava, SK .
CURRENT MEDICINAL CHEMISTRY, 2001, 8 (13) :1535-1542
[4]   Perspective in antimalarial chemotherapy [J].
Kumar, A ;
Katiyar, SB ;
Agarwal, A ;
Chauhan, PMS .
CURRENT MEDICINAL CHEMISTRY, 2003, 10 (13) :1137-1150
[5]   Current trends in antimalarial chemotherapy [J].
Kumar, A ;
Katiyar, SB ;
Agarwal, A ;
Chauhan, PMS .
DRUGS OF THE FUTURE, 2003, 28 (03) :243-255
[6]   SYNCHRONIZATION OF PLASMODIUM-FALCIPARUM ERYTHROCYTIC STAGES IN CULTURE [J].
LAMBROS, C ;
VANDERBERG, JP .
JOURNAL OF PARASITOLOGY, 1979, 65 (03) :418-420
[7]   PYRIDINE ANALOGS OF CHALCONE AND THEIR POLYMERIZATION REACTIONS [J].
MARVEL, CS ;
COLEMAN, LE ;
SCOTT, GP .
JOURNAL OF ORGANIC CHEMISTRY, 1955, 20 (12) :1785-1792
[8]   Chemotherapy of malaria [J].
Murray, MC ;
Perkins, ME .
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 31, 1996, 31 :141-150
[9]  
RIECKMANN KH, 1978, LANCET, V1, P22
[10]   Synthesis of 7-chloro-4-substituted aminoquinolines and their in vitro ability to produce methemoglobin in canine hemolysate [J].
Srivastava, S ;
Tewari, S ;
Srivastava, SK ;
Chauhan, PMS ;
Bhaduri, AP ;
Puri, SK ;
Pandey, VC .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (21) :2741-2746
123