Premium
Novel 3,6‐Disubstituted 7 H ‐1,2,4‐Triazolo[3,4‐ b ][1,3,4]thiadiazines: Synthesis, Characterization, and Evaluation of Analgesic / Anti‐inflammatory, Antioxidant Activities
Author(s) -
Tozkoparan Birsen,
Aytaç Sevim Peri,
Aktay Göknur
Publication year - 2009
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.200800188
Subject(s) - chemistry , analgesic , lipid peroxidation , anti inflammatory , antioxidant , stereochemistry , 1,2,4 triazole , chemical synthesis , structure–activity relationship , ring (chemistry) , pharmacology , medicinal chemistry , in vitro , organic chemistry , biochemistry , medicine
In this study, the synthesis of a new series of 3,6‐disubstituted‐7 H ‐1,2,4‐triazolo[3,4‐ b ][1,3,4]thiadiazine 1a – 4c compounds derived from 4‐amino‐3‐substituted‐1,2,4‐triazole‐5‐thiones 1 – 4 is described. All of the synthesized compounds were screened for their possible analgesic / anti‐inflammatory, antioxidant activities and gastric toxicity. The compound 2c was found to have both significant analgesic and consistent anti‐inflammatory activity without inducing any gastric lesions along with minimal lipid peroxidation. A deep insight into the structures of the active compounds revealed that the compounds carrying an electron withdrawing group (a chloride or fluoride) on the phenyl ring at 6‐position of the condensed heterocyclic derivatives exhibited noticeable higher activity.