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Design of Highly Potent, Dual-Acting and Central-Nervous-System-Penetrating HIV-1 Protease Inhibitors with Excellent Potency against Multidrug-Resistant HIV-1 Variants.
Ghosh AK, Rao KV, Nyalapatla PR, Kovela S, Brindisi M, Osswald HL, Sekhara Reddy B, Agniswamy J, Wang YF, Aoki M, Hattori SI, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: nyalapatla pr. ChemMedChem. 2018 Apr 23;13(8):803-815. doi: 10.1002/cmdc.201700824. Epub 2018 Mar 15. ChemMedChem. 2018. PMID: 29437300 Free PMC article.
A novel tricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor, GRL-0739, effectively inhibits the replication of multidrug-resistant HIV-1 variants and has a desirable central nervous system penetration property in vitro.
Amano M, Tojo Y, Salcedo-Gómez PM, Parham GL, Nyalapatla PR, Das D, Ghosh AK, Mitsuya H. Amano M, et al. Among authors: nyalapatla pr. Antimicrob Agents Chemother. 2015 May;59(5):2625-35. doi: 10.1128/AAC.04757-14. Epub 2015 Feb 17. Antimicrob Agents Chemother. 2015. PMID: 25691652 Free PMC article.
Design, synthesis, biological evaluation and X-ray structural studies of HIV-1 protease inhibitors containing substituted fused-tetrahydropyranyl tetrahydrofuran as P2-ligands.
Ghosh AK, Martyr CD, Kassekert LA, Nyalapatla PR, Steffey M, Agniswamy J, Wang YF, Weber IT, Amano M, Mitsuya H. Ghosh AK, et al. Among authors: nyalapatla pr. Org Biomol Chem. 2015 Dec 28;13(48):11607-21. doi: 10.1039/c5ob01930c. Epub 2015 Oct 14. Org Biomol Chem. 2015. PMID: 26462551 Free PMC article.
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
Ghosh AK, Rao KV, Nyalapatla PR, Osswald HL, Martyr CD, Aoki M, Hayashi H, Agniswamy J, Wang YF, Bulut H, Das D, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: nyalapatla pr. J Med Chem. 2017 May 25;60(10):4267-4278. doi: 10.1021/acs.jmedchem.7b00172. Epub 2017 Apr 18. J Med Chem. 2017. PMID: 28418652 Free PMC article.
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: nyalapatla pr. 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.
A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency.
Aoki M, Hayashi H, Rao KV, Das D, Higashi-Kuwata N, Bulut H, Aoki-Ogata H, Takamatsu Y, Yedidi RS, Davis DA, Hattori SI, Nishida N, Hasegawa K, Takamune N, Nyalapatla PR, Osswald HL, Jono H, Saito H, Yarchoan R, Misumi S, Ghosh AK, Mitsuya H. Aoki M, et al. Among authors: nyalapatla pr. Elife. 2017 Oct 17;6:e28020. doi: 10.7554/eLife.28020. Elife. 2017. PMID: 29039736 Free PMC article.
Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants.
Hattori SI, Hayashi H, Bulut H, Rao KV, Nyalapatla PR, Hasegawa K, Aoki M, Ghosh AK, Mitsuya H. Hattori SI, et al. Among authors: nyalapatla pr. Antimicrob Agents Chemother. 2019 May 24;63(6):e02635-18. doi: 10.1128/AAC.02635-18. Print 2019 Jun. Antimicrob Agents Chemother. 2019. PMID: 30962341 Free PMC article.
Ligand-induced Dimerization of Middle East Respiratory Syndrome (MERS) Coronavirus nsp5 Protease (3CLpro): IMPLICATIONS FOR nsp5 REGULATION AND THE DEVELOPMENT OF ANTIVIRALS.
Tomar S, Johnston ML, St John SE, Osswald HL, Nyalapatla PR, Paul LN, Ghosh AK, Denison MR, Mesecar AD. Tomar S, et al. Among authors: nyalapatla pr. J Biol Chem. 2015 Aug 7;290(32):19403-22. doi: 10.1074/jbc.M115.651463. Epub 2015 Jun 8. J Biol Chem. 2015. PMID: 26055715 Free PMC article.
17 results