title: Design and synthesis of some new quinazolin-4-(3H)-ones as anticonvulsant and antidepressant agents.
abstract: A series of 3-[(4-substituted-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-ones (5a-k) were synthesized by reacting 3-amino-2-phenyl-1H-quinazolin-4-one with p-hydroxybenzaldehyde, and then further with various alkyl/benzyl halides or substituted phenacyl bromides. The structures of the compounds were confirmed on the basis of IR, NMR, MS and elemental analysis. Anticonvulsant activities were evaluated using the MES and scPTZ tests. Some of the selected compounds were evaluated for antidepressant activity by forced swim pool test. Compound 3-[(4-butoxy-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-one was emerged as the most promising anticonvulsant agent without any motor impairment effect. The whole brain GABA estimation of brain homogenate indicated that the anticonvulsant activity of above mentioned quinazolinone derivatives might be due to an increased GABA concentration.
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi 110062, India. mamir_s2003@yahoo.co.in
authors: Mohd
authors: M
authors: Amir
authors: Israr
authors: I
authors: Ali
authors: Mohd Zaheen
authors: MZ
authors: Hassan
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004195:Disease Models, Animal; D015195:Drug Design; D051379:Mice; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013550:Swimming; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
chemical_list: D000927:Anticonvulsants; D000928:Antidepressive Agents; D011799:Quinazolines; D005680:gamma-Aminobutyric Acid