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Items: 1 to 20 of 100

1.

A novel anti-HIV active integrase inhibitor with a favorable in vitro cytochrome P450 and uridine 5'-diphospho-glucuronosyltransferase metabolism profile.

Okello MO, Mishra S, Nishonov M, Mankowski MK, Russell JD, Wei J, Hogan PA, Ptak RG, Nair V.

Antiviral Res. 2013 Jun;98(3):365-72. doi: 10.1016/j.antiviral.2013.04.005. Epub 2013 Apr 18.

2.

Approaches to the synthesis of a novel, anti-HIV active integrase inhibitor.

Okello M, Nishonov M, Singh P, Mishra S, Mangu N, Seo B, Gund M, Nair V.

Org Biomol Chem. 2013 Dec 7;11(45):7852-8. doi: 10.1039/c3ob41728j. Epub 2013 Oct 7.

3.

Notable difference in anti-HIV activity of integrase inhibitors as a consequence of geometric and enantiomeric configurations.

Okello M, Mishra S, Nishonov M, Nair V.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4112-6. doi: 10.1016/j.bmcl.2013.05.050. Epub 2013 May 23.

4.

The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.

Garvey EP, Johns BA, Gartland MJ, Foster SA, Miller WH, Ferris RG, Hazen RJ, Underwood MR, Boros EE, Thompson JB, Weatherhead JG, Koble CS, Allen SH, Schaller LT, Sherrill RG, Yoshinaga T, Kobayashi M, Wakasa-Morimoto C, Miki S, Nakahara K, Noshi T, Sato A, Fujiwara T.

Antimicrob Agents Chemother. 2008 Mar;52(3):901-8. Epub 2007 Dec 26. Erratum in: Antimicrob Agents Chemother. 2008 May;52(5):1899.

5.

Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.

Fenwick C, Amad M, Bailey MD, Bethell R, Bös M, Bonneau P, Cordingley M, Coulombe R, Duan J, Edwards P, Fader LD, Faucher AM, Garneau M, Jakalian A, Kawai S, Lamorte L, LaPlante S, Luo L, Mason S, Poupart MA, Rioux N, Schroeder P, Simoneau B, Tremblay S, Tsantrizos Y, Witvrouw M, Yoakim C.

Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44. doi: 10.1128/AAC.02719-13. Epub 2014 Mar 24.

6.

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.

Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Guare JP Jr, Egbertson MS, Vacca JP, Huff JR, Felock PJ, Witmer MV, Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen IW, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PG, Schleif WA, Cortese R, Emini E, Summa V, Holloway MK, Young SD.

Proc Natl Acad Sci U S A. 2004 Aug 3;101(31):11233-8. Epub 2004 Jul 26.

7.

A novel molecule with notable activity against multi-drug resistant tuberculosis.

Nair V, Okello MO, Mangu NK, Seo BI, Gund MG.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1269-73. doi: 10.1016/j.bmcl.2015.01.050. Epub 2015 Jan 28.

8.

In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.

Reese MJ, Savina PM, Generaux GT, Tracey H, Humphreys JE, Kanaoka E, Webster LO, Harmon KA, Clarke JD, Polli JW.

Drug Metab Dispos. 2013 Feb;41(2):353-61. doi: 10.1124/dmd.112.048918. Epub 2012 Nov 6.

9.

Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.

Jones GS, Yu F, Zeynalzadegan A, Hesselgesser J, Chen X, Chen J, Jin H, Kim CU, Wright M, Geleziunas R, Tsiang M.

Antimicrob Agents Chemother. 2009 Mar;53(3):1194-203. doi: 10.1128/AAC.00984-08. Epub 2008 Dec 22.

10.

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.

Kobayashi M, Yoshinaga T, Seki T, Wakasa-Morimoto C, Brown KW, Ferris R, Foster SA, Hazen RJ, Miki S, Suyama-Kagitani A, Kawauchi-Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T.

Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. doi: 10.1128/AAC.01209-10. Epub 2010 Nov 29.

11.

Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques.

Hazuda DJ, Young SD, Guare JP, Anthony NJ, Gomez RP, Wai JS, Vacca JP, Handt L, Motzel SL, Klein HJ, Dornadula G, Danovich RM, Witmer MV, Wilson KA, Tussey L, Schleif WA, Gabryelski LS, Jin L, Miller MD, Casimiro DR, Emini EA, Shiver JW.

Science. 2004 Jul 23;305(5683):528-32. Epub 2004 Jul 8.

12.

Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids.

Nair V, Okello M.

Molecules. 2015 Jul 13;20(7):12623-51. doi: 10.3390/molecules200712623. Review.

13.

Symmetrical 1-pyrrolidineacetamide showing anti-HIV activity through a new binding site on HIV-1 integrase.

Du L, Zhao YX, Yang LM, Zheng YT, Tang Y, Shen X, Jiang HL.

Acta Pharmacol Sin. 2008 Oct;29(10):1261-7. doi: 10.1111/j.1745-7254.2008.00863.x.

15.

Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137).

Shimura K, Kodama E, Sakagami Y, Matsuzaki Y, Watanabe W, Yamataka K, Watanabe Y, Ohata Y, Doi S, Sato M, Kano M, Ikeda S, Matsuoka M.

J Virol. 2008 Jan;82(2):764-74. Epub 2007 Oct 31.

16.

Novel HIV-1 integrase inhibitors derived from quinolone antibiotics.

Sato M, Motomura T, Aramaki H, Matsuda T, Yamashita M, Ito Y, Kawakami H, Matsuzaki Y, Watanabe W, Yamataka K, Ikeda S, Kodama E, Matsuoka M, Shinkai H.

J Med Chem. 2006 Mar 9;49(5):1506-8.

PMID:
16509568
17.

Diketo acids derivatives as integrase inhibitors: the war against the acquired immunodeficiency syndrome.

Henao-Mejia J, Góez Y, Patiño P, Rugeles MT.

Recent Pat Antiinfect Drug Discov. 2006 Jun;1(2):255-65. Review.

PMID:
18221151
18.

Bicyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.

Zhao XZ, Maddali K, Metifiot M, Smith SJ, Vu BC, Marchand C, Hughes SH, Pommier Y, Burke TR Jr.

Chem Biol Drug Des. 2012 Feb;79(2):157-65. doi: 10.1111/j.1747-0285.2011.01270.x. Epub 2011 Dec 22.

PMID:
22107736
19.

Discovery of HIV-1 integrase inhibitors: pharmacophore mapping, virtual screening, molecular docking, synthesis, and biological evaluation.

Bhatt H, Patel P, Pannecouque C.

Chem Biol Drug Des. 2014 Feb;83(2):154-66. doi: 10.1111/cbdd.12207. Epub 2013 Oct 4.

PMID:
23957390

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