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An influential method for the synthesis of imidazo[2,1‐b]thiazoles via copper (I) catalysis was advanced through a multicomponent coupling of pharmacological scaffolds involving 2‐aminothiazolyl‐coumarin, benzaldehyde, and phenyl acetylene, a concealed variation. The protocol allows the establishment of highly efficient and user‐friendly catalytic system for the A3 cascade coupling; also, an environmentally benign, economical, and readily obtainable CuSO4/sodium ascorbate is portrayed. A sequence of 15 novel imidazo[2,1‐b]thiazoles (7j–x) were synthesized and evaluated for their in vitro antimicrobial activity, in silico studies, and oral toxicity studies. The in vitro antifungal and antibacterial screening of synthesized compounds manifested favorable activity and disclosed that all these previously unknown compounds showed significant activity. Amid them, compound 7u portrayed the most effective inhibitory activity. [ABSTRACT FROM AUTHOR]

Abstract: Two series of 4-aryloxymethyl coumarins derived from the reaction of 4-bromomethyl coumarins with ethyl gallate and ethyl ester of N-Benzoyl tyrosine have been synthesized. Gallate ethers 3a–3g and tyrosine derivatives 4e–4j were most effective against Entercoccus faecalis. They were also found to be effective against Aspergillus niger and Candida albicans. Comparative docking studies with novobiocin have indicated better binding ability and higher ‘C’ score values than novobiocin. [Copyright &y& Elsevier]