Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors
Abstract
In this paper we report the design, synthesis, in-silico and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives were synthesized separately and further combined through covalent amine bond linkage. The compounds showed more inhibition towards BuChE than AChE. The compound, 4-(3-bromophenyl)-1,3-thiazol-2-amine exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, better inhibition activities towards BuChE are shown by 3-nitro, 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole produced better results against BuChE than 4-substituted counterparts.
Keywords
Full Text:
PDFISSN 2347–9825
Authors/visitors are advised to use Firefox browser for better experience of journal site.
Open Access: Researcher from developing/low economy countries can access the jorunal contents through WHO-HINARI .