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Novel pyrimidine linked acyl thiourea derivatives as potent α-amylase and proteinase K inhibitors: design, synthesis, molecular docking and ADME studies.


ABSTRACT: To discover promising therapeutic agents, novel diaryl pyrimidine linked acyl thiourea derivatives (6a-j) were designed and synthesized via straightforward and multistep synthesis. The structure of these derivatives (6a-j) was confirmed by FTIR, 1H, and 13C NMR spectroscopic techniques. The in vitro biological screening of these compounds was carried out to assess their bacterial, α-amylase, and proteinase K inhibition potential. The results manifested that the developed molecules (6a-j) possessed a remarkable inhibition potential against targeted α-amylase and proteinase K enzymes. The compounds 6j and 6g were found to be the most potent α-amylase inhibitors with IC50 values of 1.478 ± 0.051 and 1.509 ± 0.039 μM, respectively. Meanwhile, the

SUBMITTER: Zaman H 

PROVIDER: S-EPMC11492202 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature