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Synthesis, Antihypertensive Activity, and 3D‐QSAR Studies of Some New p ‐Hydroxybenzohydrazide Derivatives
Author(s) -
Bhole Ritesh P.,
Bhusari Kishore P.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000008
Subject(s) - quantitative structure–activity relationship , chemistry , isothiocyanate , stereochemistry , organic chemistry
p ‐Hydroxybenzohydrazide 2 on treatment with aromatic/aliphatic aldehyde followed by cyclization with carbon disulphide afforded compounds 4a–4n . Also, compound 2 by treatment of substituted isothiocyanate followed by the treatment of chloroacetic acid yields the corresponding compounds 6a–6i . All the test compounds were assayed for antihypertensive activity by non‐invasive blood pressure measurement and invasive blood pressure measurement methods. The test compounds showed significant antihypertensive activity. The intact compounds were subjected to 3D‐QSAR studies. The 3D‐QSAR analysis was carried out by PHASE program and a statistically reliable model with good predictive power ( r 2 = 0.98, q 2 = 0.74) was achieved. The 3D‐QSAR plots illustrated insights into the structure‐activity relationship of these compounds which may aid in the design of potent p ‐hydroxybenzohydrazide derivatives as antihypertensive agents.