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Synthesis and Local Anesthetic Activity of Some Novel N ‐[5‐(4‐Substituted)phenyl‐1,3,4‐oxadiazol‐2‐yl]‐2‐(Substituted)‐Acetamides
Author(s) -
Rajak Harish,
Kharya Murli Dhar,
Mishra Pradeep
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700146
Subject(s) - moiety , chemistry , anesthetic , oxadiazole , local anesthetic , aryl , lidocaine , acetamide , stereochemistry , combinatorial chemistry , organic chemistry , anesthesia , medicine , alkyl
A novel series of acetamides carrying substituted‐1,3,4‐oxadiazole moiety were synthesized from reaction of 5‐aryl‐2‐chloroacetamido‐1,3,4‐oxadiazoles with different secondary amines. The local anesthetic potential of the compounds was investigated using rabbit corneal reflex method and guinea pig's wheal derm method. The present work is the only one of its kind reporting local anesthetic activity in acetamide system combined with 1,3,4‐oxadiazole nucleus. Lidocaine was selected as standard drug in evaluation of local anesthetic activity of synthesized oxadiazole analogues. Compound 19 was found to possess significant local anesthetic activity in both the models employed for evaluation of local anesthetic activity. Compound 20, 23, 28, 29 and 35 also demonstrated marked local anesthetic activities. Structure‐activity relationships among synthesized compounds were also established.