title: Microwave assisted synthesis and docking study of N-(2-oxo-2-(4-oxo-2-substituted thiazolidin-3ylamino)ethyl)benzamide derivatives as anticonvulsant agents.
abstract: Herewith, we report the design and synthesis of a series of N-(2-oxo-2((4-oxo-2-substituted thiazolidin-3yl)amino)ethyl) benzamide derivatives 7(a-j) under microwave irradiation, based on four component pharmacophoric model to get structural prerequisite indispensable for anticonvulsant activity. The synthesized derivatives were investigated in maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screening. All the test compounds were administered at a dose of 30, 100 and 300 mg/kg body weight at the time interval of 0.5 h and 4 h. The compounds were also evaluated for behavioral activity and toxicity study. The compound 7 h was found to be most active in MES model. The anticonvulsant screening data shows that 65% of the compounds were found active against MES model when compared to 35% sc-PTZ model. The computational parameter such as docking study, logP determination and ADME prediction were performed to exploit the results.
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad 431001, M.S., India. Electronic address: annapratimanikalje@gmail.com.
authors.forename: Anna Pratima G
authors.initials: APG
authors.lastname: Nikalje
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad 431001, M.S., India.
authors.forename: Arfat N
authors.initials: AN
authors.lastname: Shaikh
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad 431001, M.S., India.
authors.forename: Sameer I
authors.initials: SI
authors.lastname: Shaikh
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad 431001, M.S., India.
authors.forename: Firoz A
authors.initials: FA
authors.lastname: Kalam Khan
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad 431001, M.S., India.
authors.forename: Jaiprakash N
authors.initials: JN
authors.lastname: Sangshetti
authors.affiliation: Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, M.S., India.
authors.forename: Devanand B
authors.initials: DB
authors.lastname: Shinde
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001549:Benzamides / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001665:Binding Sites; D004195:Disease Models, Animal; D006207:Half-Life; D008099:Liver / Q000473:pathology; D051379:Mice; D008872:Microwaves; D062105:Molecular Docking Simulation; D009043:Motor Activity / Q000187:drug effects; D017434:Protein Structure, Tertiary; D012640:Seizures / Q000188:drug therapy; D015222:Sodium Channels / Q000737:chemistry / Q000378:metabolism; D053778:Thiazolidines / Q000737:chemistry
chemical_list: D000927:Anticonvulsants; D001549:Benzamides; D015222:Sodium Channels; D053778:Thiazolidines
keywords: Anticonvulsant evaluation; Benzamide; Computational studies; Microwave irradiation; Thiazolidinone