SYNTHESIS AND CALCIUM-ANTAGONIST ACTIVITY OF DIALKYL 1,4-DIHYDRO-2,6-DIMETHYL-4-(NITROGENOUS HETEROARYL)-3,5-PYRIDINE DICARBOXYLATES

被引:15
作者
BARALDI, PG
BUDRIESI, R
CACCIARI, B
CHIARINI, A
GARUTI, L
GIOVANNINETTI, G
LEONI, A
ROBERTI, M
机构
关键词
D O I
10.1135/cccc19920169
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A new series of 4-(nitrogenous heteroaryl)-1,4-dihydropyridine antagonists II-XVI were synthesized and screened for inotropic, chronotropic and calcium antagonist properties, in order to evaluate the effect on pharmacological activity of replacement of the 4-aryl group of nifedipine-like drugs by heterocyclic moieties, such as quinoline, indole, carbazole and pyrazole. The most potent bradycardic compounds of the series (VIII-X, XII and XIII) elicited weak calcium antagonist activity and were stronger negative inotropic.
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页码:169 / 178
页数:10
相关论文
共 16 条
[1]  
Baraldi P.G., 1989, DRUG DES DELIVERY, V5, P13
[2]   POTENTIAL ANTITUBERCULOSIS AGENTS OF THE INDOLE SERIES [J].
DOYLE, FP ;
FERRIER, W ;
HOLLAND, DO ;
MEHTA, MD ;
NAYLER, JHC .
JOURNAL OF THE CHEMICAL SOCIETY, 1956, (AUG) :2853-2857
[3]  
GARUTI L, 1987, PHARMAZIE, V42, P378
[4]  
Garuti L, 1989, Boll Chim Farm, V128, P136
[5]  
HOF RP, 1987, AM J CARDIOL, V59, P308
[6]  
Janis RA, 1987, ADV DRUG RES, V16, P309
[7]   Syntheses in the quinoline series. II. Some derivatives of 4-methylquinoline and a study of their structures [J].
Johnson, OH ;
Hamilton, CS .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1941, 63 :2864-2867
[8]  
Kendall H E, 1987, Prog Med Chem, V24, P249, DOI 10.1016/S0079-6468(08)70424-7
[9]  
LEIR CM, 1986, Patent No. 4565872
[10]  
PH BHN, 1951, J ORG CHEM, V16, P1327