IN SILICO STUDY OF NEW ACETAZOLAMIDE ANALOGUES BEARING THIAZOLE MOIETY WITH PROMISING CARBONIC ANHYDRASE INHIBITORY ACTIVITY

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Authors: HUSSEIN I. ABDULHUSSEIN, Noor Hatef Naser
Cited by: 0
References: 36

Abstract

Objective: Cancer is the second leading cause of death worldwide. Multiple targets can be hit for cancer treatment; carbonic anhydrase enzyme XII is one of these targets because it plays a vital role in the tumour microenvironment. Methods: ADMETlab 3.0 platform used to predict (absorption, distribution, metabolism, excretion, and toxicity) characteristics, while molecular docking managed by the molecular operating environment program MOE 2015.1. Results: The molecular docking analysis revealed that all nineteen designed compounds exhibited favourable binding affinities toward carbonic anhydrase enzymes XII (PDB ID: 1JD0) and IX (PDB ID: 3IAI), and most of the designed compounds satisfy the predominant drug-likeness requirements. Conclusion: Acetazolamide's binding affinity for the carbonic anhydrase enzyme can be enhanced by including a substituted thiazole ring.

Fields of Study & Subjects

Enzyme function and inhibition Computational Drug Discovery Methods Synthesis and biological activity

Publication details

Journal / source
International Journal of Applied Pharmaceutics
Pages
162–174
Publication date
7 January 2026