Synthesis and anti-inflammatory activities of some thiazolo[3,2-a]pyrimidine derivatives

被引:210
作者
Tozkoparan, B
Ertan, M [1 ]
Kelicen, P
Demirdamar, R
机构
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Hacettepe Univ, Fac Pharm, Dept Pharmacol, TR-06100 Ankara, Turkey
来源
FARMACO | 1999年 / 54卷 / 09期
关键词
1,2,3,4-tetrahydropyrimidine-2-thiones; thiazolo[3,2-a]pyrimidines; synthesis; anti-inflammatory activity;
D O I
10.1016/S0014-827X(99)00068-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Sixteen new 2-benzylidene-7-methyl-3-oxo-5-(substituted phenyl)-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid methyl eaters (1a-4d) have been synthesized by reacting 1,2,3,4-tetrahydropyrimidine-2-thiones (1-4) with chloroacetic acid and appropriate benzaldehydes in a single step. Their structures have been proved by IR, H-1 NMR, mass spectra and elemental analysis. The compounds were tested for their anti-inflammatory activities. Test results revealed that compounds 1b, 1c, 4a and 4c exerted moderate anti-inflammatory activity at the 100 mg/kg dose level compared with indomethacin. (C) 1999 Elsevier Science S.A. All rights reserved.
引用
收藏
页码:588 / 593
页数:6
相关论文
共 23 条
[1]   SYNTHESIS AND STRUCTURAL EVALUATIONS OF THIAZOLO[3,2-A]PYRIMIDINE DERIVATIVES [J].
BALKAN, A ;
ERTAN, M ;
BURGEMEISTER, T .
ARCHIV DER PHARMAZIE, 1992, 325 (08) :499-501
[2]  
BALKAN A, 1992, PHARMAZIE, V47, P687
[3]  
Balkan A, 1996, Boll Chim Farm, V135, P648
[4]  
BIGG D, 1981, Patent No. 2479831
[5]  
BRAETZ J, 1973, Patent No. 1334628
[6]  
CHAMPANERI HR, 1994, ASIAN J CHEM, V6, P737
[7]   DIHYDROPYRIMIDINES - NOVEL CALCIUM-ANTAGONISTS WITH POTENT AND LONG-LASTING VASODILATIVE AND ANTIHYPERTENSIVE ACTIVITY [J].
CHO, H ;
UEDA, M ;
SHIMA, K ;
MIZUNO, A ;
HAYASHIMATSU, M ;
OHNAKA, Y ;
TAKEUCHI, Y ;
HAMAGUCHI, M ;
AISAKA, K ;
HIDAKA, T ;
KAWAI, M ;
TAKEDA, M ;
ISHIHARA, T ;
FUNAHASHI, K ;
SATOH, F ;
MORITA, M ;
NOGUCHI, T .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (10) :2399-2406
[8]  
Dash B., 1980, J I CHEM, V52, P92
[9]  
DEHURI SN, 1983, J INDIAN CHEM SOC, V60, P970
[10]  
DORIA G, 1985, FARMACO-ED SCI, V40, P885