Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

被引:1
作者
Zhang, Pingzhu [1 ]
Wang, Xiaofen [1 ]
Zheng, Xuevang [1 ]
Lian, Pingping [1 ]
Wei, Chao [1 ]
Li, Xiaoliu [1 ]
机构
[1] Hebei Univ, Sch Chem & Environm Sci, Minist Educ, Key Lab Chem Biol Hebei Prov,Key Lab Med Chem & M, Baoding 071002, Peoples R China
基金
中国国家自然科学基金;
关键词
Knoevenagel reaction; Biginelli reaction; imidazo[1,2-a]dihypyrimidine; imidazo[1,2-a]pyrimidine; triazolo[1,5-a]pyrimidine; CALCIUM-CHANNEL BLOCKERS; POTENT MIMICS; DIHYDROPYRIMIDINES;
D O I
10.6023/cjoc201804020
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of novel aryl-substituted imidazo[1,2-a]pyrimidine and triazolo[1,5-a] pyrimidine were synthesized by the tandem reaction of Knoevenagel and Atwal modified Biginelli, following by aromatization. Some of their cytotoxic activities against Hela and A549 cells and inhibition for apple tree canker were preliminarily evaluated.
引用
收藏
页码:3278 / 3285
页数:8
相关论文
共 23 条
[1]   Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: Synthesis and pharmacological evaluation [J].
Alam, Ozair ;
Khan, Suroor A. ;
Siddiqui, Nadeem ;
Ahsan, Waquar ;
Verma, Suraj P. ;
Gilani, Sadaf J. .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (11) :5113-5119
[2]  
Atwal K. S. EP, 1987, [No title captured], Patent No. 211429
[3]  
ATWAL KS, 1987, HETEROCYCLES, V26, P1189
[4]   DIHYDROPYRIMIDINE CALCIUM-CHANNEL BLOCKERS 51 - BICYCLIC DIHYDROPYRIMIDINES AS POTENT MIMICS OF DIHYDROPYRIDINES [J].
ATWAL, KS ;
MORELAND, S .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1991, 1 (06) :291-294
[5]   DIHYDROPYRIMIDINE CALCIUM-CHANNEL BLOCKERS - 2-HETEROSUBSTITUTED 4-ARYL-1,4-DIHYDRO-6-METHYL-5-PYRIMIDINECARBOXYLIC ACID-ESTERS AS POTENT MIMICS OF DIHYDROPYRIDINES [J].
ATWAL, KS ;
ROVNYAK, GC ;
SCHWARTZ, J ;
MORELAND, S ;
HEDBERG, A ;
GOUGOUTAS, JZ ;
MALLEY, MF ;
FLOYD, DM .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1510-1515
[6]   SUBSTITUTED 1,4-DIHYDROPYRIMIDINES .3. SYNTHESIS OF SELECTIVELY FUNCTIONALIZED 2-HETERO-1,4-DIHYDROPYRIMIDINES [J].
ATWAL, KS ;
ROVNYAK, GC ;
OREILLY, BC ;
SCHWARTZ, J .
JOURNAL OF ORGANIC CHEMISTRY, 1989, 54 (25) :5898-5907
[7]  
Biginelli P., 1891, Berichte Der Deutschen Chemischen Gesellschaft, V24, P2962, DOI 10.1002/cber.189102402126
[8]   Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors [J].
Chen, Xinde ;
Xu, Wenwei ;
Wang, Kai ;
Mo, Mingguang ;
Zhang, Wei ;
Du, Lili ;
Yuan, Xiaojing ;
Xu, Yechun ;
Wang, Yiping ;
Shen, Jianhua .
JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (21) :8529-8541
[9]  
Kappe C.O., 2004, ORGANIC REACTIONS, V63, P1, DOI [DOI 10.1002/0471264180.OR063.01, 10.1002/0471264180.or063.01]
[10]  
Kappe CO, 2005, METH PRIN MED CHEM, V52, P1, DOI 10.1002/3527606556