title: Synthesis, antihypertensive activity, and 3D-QSAR studies of some new p-hydroxybenzohydrazide derivatives.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, Sharad Pawar College of Pharmacy, Nagpur, MS, India. riteshb986@gmail.com
authors.forename: Ritesh P
authors.initials: RP
authors.lastname: Bhole
authors.forename: Kishore P
authors.initials: KP
authors.lastname: Bhusari
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D008958:Models, Molecular; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D000959:Antihypertensive Agents; D006834:Hydrazines