title: Synthesis and antihypertensive screening of new derivatives of quinazolines linked with isoxazole.
abstract: A series of 7-substituted-3-(4-(3-(4-substitutedphenyl)-4,5-dihydroisoxazol-5-yl)phenyl)-2-substituted quinazolin-4(3H)-one (1-30) have been synthesized by the cyclization of (E)-3-(4-(3-substitutedphenyl)acrylolyl)phenyl)-2-(substitutedphenyl)-7-substituted quinazolin-4-(3H)-one with hydroxylamine hydrochloride. The synthesized compounds were examined for their in vivo antihypertensive activity using albino rats. All the titled compounds exhibited good to moderate antihypertensive activity. Compounds 7-Chloro-3-(4-(3-(4-chlorophenyl)-4,5- dihydroisoxazol-5-yl)phenyl)-2-p-tolylquinazolin-4(3H)-one (23) and 7-Chloro-3-(4-(3-(4-chlorophenyl)-4,5-dihydroisoxazol-5-yl)phenyl)-2-(4-methoxyphenyl)quinazolin-4(3H)-one (24) exhibited potent antihypertensive activity through their anticipated α 1-adrenergic receptor blocking property similar to its clinically used analogue, prazosin, without affecting heart rate with prolonged duration of action when tested in adrenaline induced hypertension in anaesthetized rats.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India.
authors.forename: Mujeeb Ur
authors.initials: MU
authors.lastname: Rahman
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India.
authors.forename: Ankita
authors.initials: A
authors.lastname: Rathore
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India.
authors.forename: Anees A
authors.initials: AA
authors.lastname: Siddiqui
authors.affiliation: SunRise University, Alwar 301030, India.
authors.forename: Gazala
authors.initials: G
authors.lastname: Parveen
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India.
authors.forename: M
authors.initials: M
authors.lastname: Shahar Yar
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D004837:Epinephrine / Q000494:pharmacology; D006801:Humans; D006973:Hypertension / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D007555:Isoxazoles / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D015394:Molecular Structure; D011799:Quinazolines / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000959:Antihypertensive Agents; D007555:Isoxazoles; D011799:Quinazolines; D004837:Epinephrine