Novel quinoxaline-hydrazidehydrazone-1,2,3-triazole hybrids were synthesized, characterized and screened for α-glucosidase inhibitory and antioxidant activities.
A mixture of ethyl 5-amino-4-cyano-3-methylthiophene-2carboxylate [21] 1 (2.10 g, 10 mmol) in triethyl orthoformate (12 mL) was heated under refluxion for 14 h. After completion of starting compound, the excess amount of triethyl orthoformate was removed under vacuum. The residue was washed with petroleum ether then they obtain solid was filtered and recrystallized from DMSO water.
In pursuit of neuroprotective and antimicrobial agents, a series of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole incorporated thieno[2,3d]pyrimidine derivatives 10 a-l has been designed, synthesized. The final target compounds were screened for neuroprotective, neurotoxic and antibacterial activities. The compounds derived from 4-methylphenyl (10 a) and 4-nitrophenyl (10 c) have showed good neuroprotective activity against H 2 O 2 induced PC12 cell death at respective EC 50 values of 10.44, 14.12 μg/mL. However 10 b and 10 k showed superior neurotoxic effects than rest of the compounds with respective CC 50 values of 100.16, 120 μg/mL. Potent antibacterial activity was shown by 10 f (R =-Me, R 2 =-OMe), 10 h (R =-Me, R 2 =-Cl) against the four bacterial pathogens such as S.aureus, B.subtilis, E.coli and P.aeruginosa at low minimum inhibitory concentration (MIC) range. Further, in silico docking studies were performed for all the synthesized compounds with C(30) carotenoid dehydrosqualene synthase, Gyrase A and LpxC bacterial proteins. Interestingly, 10 f, 10 h showed good binding affinities with target proteins and these results are in good compliance with the in vitro activity profile data.
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