Poornima Acharya, M.M.V. Ramana*, Manish Upadhyay and Ganesh Pavale Pages 57 - 66 ( 10 )
Background: Biscoumarin scaffolds are known for their promising pharmacological properties. These compounds have not been studied for their activity against tuberculosis strains.Objective: Unveil the antitubercular properties of biscoumarin scaffolds. Methods: Biscoumarin derivatives (3a-3l) were synthesized using lemon juice as a catalyst and were investigated for their in-vitro anti-tubercular activity against the H37Rv strain of Mycobacterium tuberculosis using Microplate Alamar Blue Assay Method (MABA). Their binding interaction was investigated by Molecular Docking Studies using InhA with PDB-ID: 2NSD as target receptors in the H37Rv strain of Mycobacterium tuberculosis. These derivatives (3a-3l) were subjected to the neutrophil function test. Results: The results revealed that compounds 3b, 3c, 3d, 3f, 3i, 3j showed excellent activity with MIC 1.6μg/mL. Molecular docking interactions for their antitubercular activity proved that the derivatives (3a-3l) can easily bind into the pockets of the enzyme. Neutrophil function test signified that they exhibit moderate neutrophil functions assuring that they do not harm the functioning of Neutrophils. Conclusion: These studies have awakened the property of Biscoumarins as promising antitubercular scaffolds.
Biscoumarin, Mycobacterium tuberculosis, microplate alamar blue assay method, InhA, neutrophil function test, ADME.
Department of Chemistry, University of Mumbai, Vidyanagari, Santacruz (E), Mumbai-400 098, Department of Chemistry, University of Mumbai, Vidyanagari, Santacruz (E), Mumbai-400 098, Department of Bioinformatic, Guru Nanak Khalsa College, University of Mumbai, Mumbai, Department of Chemistry, University of Mumbai, Vidyanagari, Santacruz (E), Mumbai-400 098