Comparative QSAR studies of two series of 1,4-dihydropyridines as slow calcium channel blockers

Autor: J H, Wikel, K G, Bemis, K, Kurz, M L, Denney, B W, Main, R A, Moore, T, Smith, L, Shingleton, D R, Holland
Rok vydání: 1994
Předmět:
Zdroj: Drug design and discovery. 11(1)
ISSN: 1055-9612
Popis: Quantitative structure activity analysis was applied to two series of dihydropyridine (DHP) calcium channel blocking agents. One series of compounds was composed of DHPs substituted in the 4-position with an ortho or meta nitro substituted phenyl ring. The second group consisted of DHPs substituted at the 4-position with a novel thieno [3,2-c] pyridine ring. Both series consisted of compounds with unsymmetrical ester substitutions on the dihydropyridine ring. The antihypertensive activity of the compounds were determined in a spontaneously hypertensive rat model. Regression analysis indicated the antihypertensive activity of an i.v. dose correlated with the calculated octanol/water coefficent (clogP). Regression analysis did not find correlation with the in vitro potency and the clogP values.
Databáze: OpenAIRE