Litcius/Paper detail

2-Benzylidenebenzofuran-3(2<i>H</i>)-ones as a new class of alkaline phosphatase inhibitors: synthesis, SAR analysis, enzyme inhibitory kinetics and computational studies

Jamshaid Ashraf, Ehsan Ullah Mughal, Reem I. Alsantali, Amina Sadiq, Rabab S. Jassas, Nafeesa Naeem, Zaman Ashraf, Yasir Nazir, Muhammad Naveed Zafar, Amara Mumtaz, Masoud Mirzaei, Satar Saberi, Saleh A. Ahmed

2021RSC Advances31 citationsDOIOpen Access PDF

Abstract

a non-competitive pathway. Finally, molecular dynamic (MD) simulations were performed to evaluate the dynamic behavior, stability of the protein-ligand complex, and binding affinity of the compounds, resulting in the identification of compound 20 as a potential inhibitor of AP. Accordingly, excellent correlation was observed between the experimental and theoretical results. The pharmacological studies revealed that the synthesized analogs 1-22 obey Lipinski's rule. The assessment of the ADMET parameters showed that these compounds possess considerable lead-like characteristics with low toxicity and can serve as templates in drug design.

Topics & Concepts

KineticsAlkaline phosphataseInhibitory postsynaptic potentialChemistryEnzymeEnzyme kineticsClass (philosophy)PhosphataseEnzyme inhibitionStereochemistryBiochemistryCombinatorial chemistryActive siteBiologyComputer sciencePhysicsEndocrinologyArtificial intelligenceQuantum mechanicsAlkaline Phosphatase Research StudiesSynthesis and Characterization of Heterocyclic CompoundsSynthesis and Reactivity of Heterocycles