2. Academic Validation
  3. Design, Synthesis, and Biological Evaluation of Densely Substituted Dihydropyrano[2,3- c]pyrazoles via a Taurine-Catalyzed Green Multicomponent Approach

Design, Synthesis, and Biological Evaluation of Densely Substituted Dihydropyrano[2,3- c]pyrazoles via a Taurine-Catalyzed Green Multicomponent Approach

  • ACS Omega. 2021 Nov 2;6(45):30734-30742. doi: 10.1021/acsomega.1c04773.
Ghanshyam Mali 1,  Badrodin A Shaikh 2,  Shivani Garg 3,  Akhilesh Kumar 4,  Sudipta Bhattacharyya 3,  Rohan D Erande 1,  Asha V Chate 2
Affiliations

Affiliations

  • 1 Department of Chemistry, Indian Institute of Technology Jodhpur, Jodhpur 342037, India.
  • 2 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, India.
  • 3 Department of Bioscience and Bioengineering, Indian Institute of Technology Jodhpur, Jodhpur 342037, India.
  • 4 Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016, India.
PMID: 34805701 DOI: 10.1021/acsomega.1c04773
Abstract

An efficient taurine-catalyzed green multicomponent approach has been described for the first time to synthesize densely substituted therapeutic core dihydropyrano[2,3-c]pyrazoles. Applications of the developed synthetic strategies and technologies revealed the synthesis of a series of newly designed 1,4-dihydropyrano[2,3-c]pyrazoles containing isonicotinamide, spirooxindole, and indole moieties. Detailed in silico analysis of the synthesized analogues revealed their potential to bind wild-type and antibiotic-resistant variants of dihydrofolate reductase, a principal drug target Enzyme for emerging antibiotic-resistant pathogenic Staphylococcus aureus strains. Hence, the synthesized dihydropyrano[2,3-c]pyrazole derivatives presented herein hold immense promise to develop future antistaphylococcal therapeutic agents.

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