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Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.

Ghosh AK, Sean Fyvie W, Brindisi M, Steffey M, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H
Bioorg Med Chem Lett 27 4925-4931 (2017)
Cited: 5 times
EuropePMC logo PMID: 28958624

Abstract

Design, synthesis, and evaluation of a new class of HIV-1 protease inhibitors containing diverse flexible macrocyclic P1'-P2' tethers are reported. Inhibitor 5a with a pyrrolidinone-derived macrocycle exhibited favorable enzyme inhibitory and antiviral activity (Ki=13.2nM, IC50=22nM). Further incorporation of heteroatoms in the macrocyclic skeleton provided macrocyclic inhibitors 5m and 5o. These compounds showed excellent HIV-1 protease inhibitory (Ki=62pM and 14pM, respectively) and antiviral activity (IC50=5.3nM and 2.0nM, respectively). Inhibitor 5o also remained highly potent against a DRV-resistant HIV-1 variant.

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  2. Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands. Ghosh AK, Sean Fyvie W, Brindisi M, Steffey M, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H. Bioorg Med Chem Lett 27 4925-4931 (2017)


Reviews citing this publication (1)

  1. Proteases: Pivot Points in Functional Proteomics. Verhamme IM, Leonard SE, Perkins RC. Methods Mol Biol 1871 313-392 (2019)

Articles citing this publication (2)

  1. Recognition of Divergent Viral Substrates by the SARS-CoV-2 Main Protease. MacDonald EA, Frey G, Namchuk MN, Harrison SC, Hinshaw SM, Windsor IW. ACS Infect Dis 7 2591-2595 (2021)
  2. Diversity-Oriented Synthesis of Diol-Based Peptidomimetics as Potential HIV Protease Inhibitors and Antitumor Agents. Vadhadiya PM, Jean MA, Bouzriba C, Tremblay T, Lagüe P, Fortin S, Boukouvalas J, Giguère D. Chembiochem (2018)


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