2. Academic Validation
  3. Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs

Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs

  • Bioorg Med Chem. 2022 Feb 15;56:116612. doi: 10.1016/j.bmc.2022.116612.
Prem Kumar Kushwaha 1,  Kumar Saurabh Srivastava 2,  Neha Kumari 1,  Rajan Kumar 1,  Debashis Mitra 3,  Ashoke Sharon 4
Affiliations

Affiliations

  • 1 Department of Chemistry, Birla Institute of Technology, Mesra, Ranchi 835215, India.
  • 2 National Centre for Cell Science, SP Pune University Campus, Ganeshkhind, Pune 411007, India.
  • 3 National Centre for Cell Science, SP Pune University Campus, Ganeshkhind, Pune 411007, India. Electronic address: [email protected].
  • 4 Department of Chemistry, Birla Institute of Technology, Mesra, Ranchi 835215, India. Electronic address: [email protected].
PMID: 35026631 DOI: 10.1016/j.bmc.2022.116612
Abstract

Continuing on our Antiviral drug discovery research, we intended to diversify our lead anti-HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles. The resulting molecules isoxazole-1,2,4-oxadiazole analogs were synthesized using mild bases in ethanol under microwave irradiation. The anti-HIV potential was checked in human CD4+ reporter cell lines, TZM-bl and CEM-GFP, at the highest non-cytotoxic concentration (HNC), demonstrating that 3-((3-(p-tolyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole and 3-((3-(4-chlorophenyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole inhibit HIV-1 replication significantly and could be considered as a new lead candidate against HIV-1.

Keywords

2; 4-oxadiazoles; Bioisosteres; HIV-1 inhibitors; Isoxazole-1; Microwave irradiation.

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