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Bioisosteric Replacement as a Tool in Anti-HIV Drug Design

Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Rooms 10307, 10309, and 10315, 245 North 15th Street, Philadelphia, PA 19102, USA
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Pharmaceuticals 2020, 13(3), 36; https://doi.org/10.3390/ph13030036
Received: 3 February 2020 / Revised: 25 February 2020 / Accepted: 26 February 2020 / Published: 28 February 2020
(This article belongs to the Special Issue Recent Effective Application of Bioisosterism)
Bioisosteric replacement is a powerful tool for modulating the drug-like properties, toxicity, and chemical space of experimental therapeutics. In this review, we focus on selected cases where bioisosteric replacement and scaffold hopping have been used in the development of new anti-HIV-1 therapeutics. Moreover, we cover field-based, computational methodologies for bioisosteric replacement, using studies from our group as an example. It is our hope that this review will serve to highlight the utility and potential of bioisosteric replacement in the continuing search for new and improved anti-HIV drugs. View Full-Text
Keywords: bioisosteres; HIV-1; antiviral; computer-aided drug design; envelope; reverse transcriptase; protease; integrase; tat; Vif bioisosteres; HIV-1; antiviral; computer-aided drug design; envelope; reverse transcriptase; protease; integrase; tat; Vif
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Dick, A.; Cocklin, S. Bioisosteric Replacement as a Tool in Anti-HIV Drug Design. Pharmaceuticals 2020, 13, 36.

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