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Items: 1 to 20 of 244

1.

Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.

Ghosh AK, Sean Fyvie W, Brindisi M, Steffey M, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4925-4931. doi: 10.1016/j.bmcl.2017.09.003. Epub 2017 Sep 6.

2.

Design, Synthesis, Biological Evaluation, and X-ray Studies of HIV-1 Protease Inhibitors with Modified P2' Ligands of Darunavir.

Ghosh AK, Fyvie WS, Brindisi M, Steffey M, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H.

ChemMedChem. 2017 Dec 7;12(23):1942-1952. doi: 10.1002/cmdc.201700614. Epub 2017 Nov 24.

3.

Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.

Ghosh AK, Kulkarni S, Anderson DD, Hong L, Baldridge A, Wang YF, Chumanevich AA, Kovalevsky AY, Tojo Y, Amano M, Koh Y, Tang J, Weber IT, Mitsuya H.

J Med Chem. 2009 Dec 10;52(23):7689-705. doi: 10.1021/jm900695w.

4.

Synthesis of P1'-functionalized macrocyclic transition-state mimicking HIV-1 protease inhibitors encompassing a tertiary alcohol.

De Rosa M, Unge J, Motwani HV, Rosenquist Å, Vrang L, Wallberg H, Larhed M.

J Med Chem. 2014 Aug 14;57(15):6444-57. doi: 10.1021/jm500434q. Epub 2014 Aug 1.

PMID:
25054811
5.

Design and synthesis of P1-P3 macrocyclic tertiary-alcohol-comprising HIV-1 protease inhibitors.

Joshi A, Véron JB, Unge J, Rosenquist Å, Wallberg H, Samuelsson B, Hallberg A, Larhed M.

J Med Chem. 2013 Nov 27;56(22):8999-9007. doi: 10.1021/jm400811d. Epub 2013 Nov 11.

6.

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.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4903-4909. doi: 10.1016/j.bmcl.2015.05.052. Epub 2015 May 30.

7.

Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis.

Ghosh AK, R Nyalapatla P, Kovela S, Rao KV, Brindisi M, Osswald HL, Amano M, Aoki M, Agniswamy J, Wang YF, Weber IT, Mitsuya H.

J Med Chem. 2018 May 24;61(10):4561-4577. doi: 10.1021/acs.jmedchem.8b00298. Epub 2018 May 15.

8.

Symmetric fluoro-substituted diol-based HIV protease inhibitors. Ortho-fluorinated and meta-fluorinated P1/P1'-benzyloxy side groups significantly improve the antiviral activity and preserve binding efficacy.

Lindberg J, Pyring D, Löwgren S, Rosenquist A, Zuccarello G, Kvarnström I, Zhang H, Vrang L, Classon B, Hallberg A, Samuelsson B, Unge T.

Eur J Biochem. 2004 Nov;271(22):4594-602.

9.

Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.

Ali A, Reddy GS, Cao H, Anjum SG, Nalam MN, Schiffer CA, Rana TM.

J Med Chem. 2006 Dec 14;49(25):7342-56.

PMID:
17149864
10.

Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.

Ghosh AK, Leshchenko-Yashchuk S, Anderson DD, Baldridge A, Noetzel M, Miller HB, Tie Y, Wang YF, Koh Y, Weber IT, Mitsuya H.

J Med Chem. 2009 Jul 9;52(13):3902-14. doi: 10.1021/jm900303m.

11.

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.

ChemMedChem. 2015 Jan;10(1):107-15. doi: 10.1002/cmdc.201402358. Epub 2014 Oct 21.

12.

Structure-based design of potent HIV-1 protease inhibitors with modified P1-biphenyl ligands: synthesis, biological evaluation, and enzyme-inhibitor X-ray structural studies.

Ghosh AK, Yu X, Osswald HL, Agniswamy J, Wang YF, Amano M, Weber IT, Mitsuya H.

J Med Chem. 2015 Jul 9;58(13):5334-43. doi: 10.1021/acs.jmedchem.5b00676. Epub 2015 Jun 24.

13.

Design of HIV-1 protease inhibitors with C3-substituted hexahydrocyclopentafuranyl urethanes as P2-ligands: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.

Ghosh AK, Chapsal BD, Parham GL, Steffey M, Agniswamy J, Wang YF, Amano M, Weber IT, Mitsuya H.

J Med Chem. 2011 Aug 25;54(16):5890-901. doi: 10.1021/jm200649p. Epub 2011 Jul 29.

14.

Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.

Reddy GS, Ali A, Nalam MN, Anjum SG, Cao H, Nathans RS, Schiffer CA, Rana TM.

J Med Chem. 2007 Sep 6;50(18):4316-28. Epub 2007 Aug 16.

15.

Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.

Yang ZH, Bai XG, Zhou L, Wang JX, Liu HT, Wang YC.

Bioorg Med Chem Lett. 2015 May 1;25(9):1880-3. doi: 10.1016/j.bmcl.2015.03.047. Epub 2015 Mar 24.

PMID:
25838144
16.

Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies.

Ghosh AK, Williams JN, Ho RY, Simpson HM, Hattori SI, Hayashi H, Agniswamy J, Wang YF, Weber IT, Mitsuya H.

J Med Chem. 2018 Nov 8;61(21):9722-9737. doi: 10.1021/acs.jmedchem.8b01227. Epub 2018 Oct 24.

17.

Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.

Rodgers JD, Johnson BL, Wang H, Erickson-Viitanen S, Klabe RM, Bacheler L, Cordova BC, Chang CH.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):715-20.

PMID:
9871528
18.
19.

Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease.

Dewdney TG, Wang Y, Liu Z, Sharma SK, Reiter SJ, Brunzelle JS, Kovari IA, Woster PM, Kovari LC.

Bioorg Med Chem. 2013 Dec 1;21(23):7430-4. doi: 10.1016/j.bmc.2013.09.045. Epub 2013 Sep 27.

PMID:
24128815
20.

Unexpected binding mode of a cyclic sulfamide HIV-1 protease inhibitor.

Bäckbro K, Löwgren S, Osterlund K, Atepo J, Unge T, Hultén J, Bonham NM, Schaal W, Karlén A, Hallberg A.

J Med Chem. 1997 Mar 14;40(6):898-902.

PMID:
9083478

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