Novel Protease Inhibitors Containing C-5-Modifiedbis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2′ Ligands That Exert Potent Antiviral Activity against Highly Multidrug-Resistant HIV-1 with a High Genetic Barrier against the Emergence of Drug Resistance | Zendy

Yuki Takamatsu | Zendy; Manabu Aoki | Zendy; Haydar Bulut | Zendy; Debananda Das | Zendy; Masayuki Amano | Zendy; Venkata Reddy Sheri | Zendy; Ladislau C. Kovari | Zendy; Hironori Hayashi | Zendy; Nicole S. Delino | Zendy; Arun K. Ghosh | Zendy; Hiroaki Mitsuya | Zendy

Open Access

Novel Protease Inhibitors Containing C-5-Modifiedbis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2′ Ligands That Exert Potent Antiviral Activity against Highly Multidrug-Resistant HIV-1 with a High Genetic Barrier against the Emergence of Drug Resistance

Author(s) -

Yuki Takamatsu,

Manabu Aoki,

Haydar Bulut,

Debananda Das,

Masayuki Amano,

Venkata Reddy Sheri,

Ladislau C. Kovari,

Hironori Hayashi,

Nicole S. Delino,

Arun K. Ghosh,

Hiroaki Mitsuya

Publication year - 2019

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00372-19

Subject(s) - darunavir , protease , ritonavir , human immunodeficiency virus (hiv) , protease inhibitor (pharmacology) , pharmacology , multiple drug resistance , drug , medicine , virology , antiretroviral therapy , drug resistance , biology , viral load , microbiology and biotechnology , enzyme , biochemistry

Combination antiretroviral therapy has achieved dramatic reductions in the mortality and morbidity in people with HIV-1 infection. Darunavir (DRV) represents a most efficacious and well-tolerated protease inhibitor (PI) with a high genetic barrier to the emergence of drug-resistant HIV-1. However, highly DRV-resistant variants have been reported in patients receiving long-term DRV-containing regimens.

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