Facile and Solvent-free Domino Synthesis of New Quinolidinyl-2,4- thiazolidinones: Antifungal Activity and Molecular Docking.

Autor: Subhedar DD; Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431004, India., Shaikh MH; Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431004, India., Tupe SG; Biochemical Sciences Division, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune, 411 008, India., Deshpande MV; Biochemical Sciences Division, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune, 411 008, India., Khedkar VM; School of Health Sciences, University of KwaZulu Natal, Westville Campus, Durban, 4000, South Africa., Jha PC; School of Chemical Sciences, Central University of Gujarat, Sector-30, Gandhinagar, 38200, Gujarat, India., Shingate BB; Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431004, India.
Jazyk: angličtina
Zdroj: Mini reviews in medicinal chemistry [Mini Rev Med Chem] 2018; Vol. 18 (7), pp. 622-630.
DOI: 10.2174/1389557516666161226161152
Abstrakt: Objective: We have synthesized new quinolidinyl-thiazolidinones via Knoevenagel condensation- alkylation reaction, catalyzed by [Et3NH][HSO4]. The present approach offers several advantages such as higher yields, eco-friendly reaction condition and economic availability of the catalyst.
Method: The newly synthesized compounds were evaluated for their in vitro antifungal activity against six fungal strains. Some of the synthesized conjugates displayed good to moderate antifungal activity.
Conclusion: Again, the molecular docking study performed against the fungal sterol 14α-demethylase (CYP51) showed an excellent binding affinity towards the enzyme which could rationalize the promising antifungal activity portrayed by these derivatives and provides a platform for structure based drug design.
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Databáze: MEDLINE
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