A novel series of 2,5-disubstituted 1,3,4-oxadiazoles: synthesis and SAR study for their anticonvulsant activity.
In search for a better anticonvulsant drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4-oxadiazoles as anticonvulsant pharmacophore, a series of novel substituted semicarbazones were designed, synthesized, and evaluated for their anticonvulsant activity. The chemical structures of the synthesized molecules were confirmed by elemental and spectral (IR, (1) H NMR, (13) C NMR and MS) analysis. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure and subcutaneous pentylenetetrazole (scPTZ) models. Efforts were also made to establish structure-activity relationships among synthesized compounds. The results of the present study validated that the pharmacophore model with four binding sites is essential for anticonvulsant activity.
SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur 495 009, Chhattisgarh, India. harishdops@yahoo.co.in
Harish
H
Rajak
Pradeep
P
Singour
Murli Dhar
MD
Kharya
Pradeep
P
Mishra
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D004195:Disease Models, Animal; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D008968:Molecular Conformation; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D010433:Pentylenetetrazole / Q000633:toxicity; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D010069:Oxadiazoles; D012664:Semicarbazones; D010433:Pentylenetetrazole