A novel series of thiazole-triazole-piperazine multi hybrids was designed for antimicrobial activity
and the synthetic method for this series has been developed by copper catalyzed 1,3-dipolar
cycloaddition of thiazole-based azide with Boc-piperidine based alkyne in the presence of CuSO4 and
sodium ascorbate. Boc deprotection followed by alkylation of piperidine moiety in hybrid derivatives
was also carried out. All the target compounds were confirmed using FTIR, 1H NMR, 13C NMR and
LC-MS spectral techniques. These compounds were screened for the antimicrobial activity against
bacteria and fungi. The antimicrobial activities are also comparable to standard drugs ampicillin and
clotrimazole. All the molecules showed good to moderate activity and supported by molecular docking
studies and ADME prediction.
Novel series of fused heterocycles in which amino triazole fused to biphenyl thiazole were synthesized
in a multistep reaction starting from 2-aminothiazole. The amino compound with ethoxy carbonyl
isothiocyanate afforded the ethyl carbamate thiomide derivative of thiazole, which further underwent
intramolecular cyclization with hydroxyl amine hydrochloride in presence of DIPEA to furnish the
fused thiazolotriazole amine. Haloaryl group in the fused heterocycle under Suzuki coupling condition
afforded biphenyl derivatives of fused thiazolotriazole amines. All the synthesized compounds were
confirmed based on their spectral data.
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