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Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex.
Ghosh AK, Brindisi M, Nyalapatla PR, Takayama J, Ella-Menye JR, Yashchuk S, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: yashchuk s. Bioorg Med Chem. 2017 Oct 1;25(19):5114-5127. doi: 10.1016/j.bmc.2017.04.005. Epub 2017 Apr 9. Bioorg Med Chem. 2017. PMID: 28434781 Free PMC article.
GRL-04810 and GRL-05010, difluoride-containing nonpeptidic HIV-1 protease inhibitors (PIs) that inhibit the replication of multi-PI-resistant HIV-1 in vitro and possess favorable lipophilicity that may allow blood-brain barrier penetration.
Salcedo Gómez PM, Amano M, Yashchuk S, Mizuno A, Das D, Ghosh AK, Mitsuya H. Salcedo Gómez PM, et al. Among authors: yashchuk s. Antimicrob Agents Chemother. 2013 Dec;57(12):6110-21. doi: 10.1128/AAC.01420-13. Epub 2013 Sep 30. Antimicrob Agents Chemother. 2013. PMID: 24080647 Free PMC article.
Design of gem-difluoro-bis-tetrahydrofuran as P2 ligand for HIV-1 protease inhibitors to improve brain penetration: synthesis, X-ray studies, and biological evaluation.
Ghosh AK, Yashchuk S, Mizuno A, Chakraborty N, Agniswamy J, Wang YF, Aoki M, Gomez PM, Amano M, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: yashchuk s. ChemMedChem. 2015 Jan;10(1):107-15. doi: 10.1002/cmdc.201402358. Epub 2014 Oct 21. ChemMedChem. 2015. PMID: 25336073 Free PMC article.
Structure-based design, synthesis, X-ray studies, and biological evaluation of novel HIV-1 protease inhibitors containing isophthalamide-derived P2-ligands.
Ghosh AK, Takayama J, Kassekert LA, Ella-Menye JR, Yashchuk S, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: yashchuk s. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4903-4909. doi: 10.1016/j.bmcl.2015.05.052. Epub 2015 May 30. Bioorg Med Chem Lett. 2015. PMID: 26096678 Free PMC article.