title: Synthesis and antiepileptic activity of some novel semicarbazones containing 1,3,4-thiadiazole and quinazoline ring.
abstract: The incomplete seizure control with frequent adverse effects of current anticonvulsant drugs and the importance of semicarbazones, quinazolines and 2,5-disubstituted 1,3,4-thiadiazoles as anticonvulsant pharmacophore prompted us to carry out synthesis of three novel series of semicarbazones containing 1,3,4-thiadiazole and quinazoline ring. The chemical structures of these compounds were elucidated by elemental and spectral (IR, 1H NMR, 13C NMR and MS) analysis. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) models. The rotorod test was conducted to evaluate neurotoxicity. The majority of the compounds were found active in the biological screening. The outcome of the present investigations proved that the four binding sites pharmacophore model is decisive for antiepileptic activity. An attempt has also been performed to establish structure-activity relationships among synthesized compounds.
authors.affiliation: Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur-495 009, India. harishdops@yahoo.co.in
authors.forename: Harish
authors.initials: H
authors.lastname: Rajak
authors.forename: Bhupendra S
authors.initials: BS
authors.lastname: Thakur
authors.forename: Pramod
authors.initials: P
authors.lastname: Kumar
authors.forename: Poonam
authors.initials: P
authors.lastname: Parmar
authors.forename: Prabodh Chander
authors.initials: PC
authors.lastname: Sharma
authors.forename: Ravichandran
authors.initials: R
authors.lastname: Veerasamy
authors.forename: Murli Dhar
authors.initials: MD
authors.lastname: Kharya
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000927:Anticonvulsants; D011799:Quinazolines; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole