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Chemical structures of FDA-approved HIV-1 protease inhibitors Ritonavir and Darunavir.

Journal: ACS Omega

Article Title: Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies

doi: 10.1021/acsomega.5c09361

Figure Lengend Snippet: Chemical structures of FDA-approved HIV-1 protease inhibitors Ritonavir and Darunavir.

Article Snippet: Darunavir was purchased from MedChemExpress (HY-17040, New Jersey, USA).

Techniques:

In vitro inhibitory activity of PACs. A) Relative activities of Darunavir and PACs at 1 μM, 100 nM and 10 nM. The bars represent means ± SD, n = 2. B) PAC-Phe-Val ( 9c ) inhibited the activity of HIV-1 protease. The bars represent means ± SD, n = 3. C) Relative activities of the three isolated isomers of PAC-Phe-Val ( 9c ) and Darunavir at 1 μM, 100 nM and 10 nM. D) Isomer 1 of PAC-Phe-Val ( 9c ) inhibited the activity of HIV-1 protease. The bars represent means ± SD, n = 3.

Journal: ACS Omega

Article Title: Highly Potent Phosphinic HIV‑1 Protease Inhibitors: Synthesis, In Vitro Evaluation, and Docking Studies

doi: 10.1021/acsomega.5c09361

Figure Lengend Snippet: In vitro inhibitory activity of PACs. A) Relative activities of Darunavir and PACs at 1 μM, 100 nM and 10 nM. The bars represent means ± SD, n = 2. B) PAC-Phe-Val ( 9c ) inhibited the activity of HIV-1 protease. The bars represent means ± SD, n = 3. C) Relative activities of the three isolated isomers of PAC-Phe-Val ( 9c ) and Darunavir at 1 μM, 100 nM and 10 nM. D) Isomer 1 of PAC-Phe-Val ( 9c ) inhibited the activity of HIV-1 protease. The bars represent means ± SD, n = 3.

Article Snippet: Darunavir was purchased from MedChemExpress (HY-17040, New Jersey, USA).

Techniques: In Vitro, Activity Assay, Isolation