Synthesis,characterization and pharmacological evaluation of some new 1,3,4-oxadiazole derivatives bearing 3-chloro-2-fluoro phenyl moiety |
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| Authors: | Manjunatha Bhat G K Nagaraja Reshma Kayarmar S V Raghavendra K P Rajesh H Manjunatha |
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| Institution: | 1.Department of Post Graduate Studies and Research in Chemistry,Mangalore University,Mangalagangothri, Mangalore,India;2.SeQuent Scientific Limited,Baikampady, New Mangalore,India;3.Dayanand Sagar College of Pharmacy,Bangalore,India;4.Department of PG Studies and Research in Biotechnology and Bioinformatics,Kuvempu University,Jnanasahyadri, Shankaraghatta,India |
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| Abstract: | A new series of 2-(3-chloro-2-fluorophenyl)-5-aryl-1,3,4-oxadiazole (3a–j) and 2-(aryl sulfanyl)-5-(3-chloro-2-fluorophenyl)-1,3,4-oxadiazole (5a–e) were synthesized via a multistep reaction from 3-chloro-2-fluoro benzoic acid. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. They were also screened for their in vivo anti-convulsant and anti-inflammatory activities. Some of them exhibited significant biological activities and were well supported by in silico molecular docking studies for the inhibition of cyclooxygenase-2 (PDB ID: 1CX2) and voltage-gated sodium channels (PDB ID: 4F4L) comparable with the standard drugs. Thus, they were believed to be good inhibitors of cyclooxygenase-2 (PDB ID: 1CX2) and voltage-gated sodium channels (PDB ID: 4F4L). |
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