title: Synthesis and characterization of quinazoline derivatives: search for hybrid molecule as diuretic and antihypertensive agents.
abstract: To explore the pharmacological and structure-activity relationship of a series of N-substituted-(4-oxo-2-substituted-phenylquinazolin-3-(4H)-yl), substituted benzene sulfonamide derivatives (1-25) were synthesized from substituted anthranilic acids derived amino quinazolines and substituted benzene sulphonamides. All the synthesized compounds were evaluated for their diuretic (by Lipschitz et al. method), antihypertensive activity by non-invasive blood pressure (NIBP) using the tail-cuff method and anti-diabetic potential in rats. Six compounds showing significantly excellent activity were compared with metolazone, prazosin and diazoxide as standards. Compound N-[7-chloro-2-(4-methoxyphenyl)-4-oxoquinazolin-3(4H)-yl]-4 nitrobenzenesulfonamide (20) exhibited most potent of the series.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) , Hamdard Nagar, New Delhi , India and.
authors.lastname: Mujeeb Ur Rahman
authors.forename: Ankita
authors.initials: A
authors.lastname: Rathore
authors.forename: Anees A
authors.initials: AA
authors.lastname: Siddiqui
authors.forename: Gazala
authors.initials: G
authors.lastname: Parveen
authors.forename: M Shahar
authors.initials: MS
authors.lastname: Yar
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004232:Diuretics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006973:Hypertension / Q000188:drug therapy*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000959:Antihypertensive Agents; D004232:Diuretics; D007004:Hypoglycemic Agents; D011799:Quinazolines
keywords: Anti-diabetic potential; antihypertensive activity; diuretic activity; quinazoline