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 |
Externí odkaz: |
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