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Items: 1 to 20 of 81

1.

Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).

Johns BA, Kawasuji T, Weatherhead JG, Taishi T, Temelkoff DP, Yoshida H, Akiyama T, Taoda Y, Murai H, Kiyama R, Fuji M, Tanimoto N, Jeffrey J, Foster SA, Yoshinaga T, Seki T, Kobayashi M, Sato A, Johnson MN, Garvey EP, Fujiwara T.

J Med Chem. 2013 Jul 25;56(14):5901-16. doi: 10.1021/jm400645w. Epub 2013 Jul 11.

PMID:
23845180
2.

Carbamoyl pyridone HIV-1 integrase inhibitors. 2. Bi- and tricyclic derivatives result in superior antiviral and pharmacokinetic profiles.

Kawasuji T, Johns BA, Yoshida H, Weatherhead JG, Akiyama T, Taishi T, Taoda Y, Mikamiyama-Iwata M, Murai H, Kiyama R, Fuji M, Tanimoto N, Yoshinaga T, Seki T, Kobayashi M, Sato A, Garvey EP, Fujiwara T.

J Med Chem. 2013 Feb 14;56(3):1124-35. doi: 10.1021/jm301550c. Epub 2013 Jan 22.

PMID:
23316884
3.

The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.

Siu T, Kozina ES, Jung J, Rosenstein C, Mathur A, Altman MD, Chan G, Xu L, Bachman E, Mo JR, Bouthillette M, Rush T, Dinsmore CJ, Marshall CG, Young JR.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7421-5. doi: 10.1016/j.bmcl.2010.10.031. Epub 2010 Oct 12.

PMID:
21044843
4.

An efficient and highly diastereoselective synthesis of GSK1265744, a potent HIV integrase inhibitor.

Wang H, Kowalski MD, Lakdawala AS, Vogt FG, Wu L.

Org Lett. 2015 Feb 6;17(3):564-7. doi: 10.1021/ol503580t. Epub 2015 Jan 23.

PMID:
25615910
5.

Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase.

Verschueren WG, Dierynck I, Amssoms KI, Hu L, Boonants PM, Pille GM, Daeyaert FF, Hertogs K, Surleraux DL, Wigerinck PB.

J Med Chem. 2005 Mar 24;48(6):1930-40.

PMID:
15771437
6.

Carbamoyl pyridone HIV-1 integrase inhibitors. 1. Molecular design and establishment of an advanced two-metal binding pharmacophore.

Kawasuji T, Johns BA, Yoshida H, Taishi T, Taoda Y, Murai H, Kiyama R, Fuji M, Yoshinaga T, Seki T, Kobayashi M, Sato A, Fujiwara T.

J Med Chem. 2012 Oct 25;55(20):8735-44. doi: 10.1021/jm3010459. Epub 2012 Oct 4.

PMID:
22963135
7.

Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Johnson TW, Tanis SP, Butler SL, Dalvie D, Delisle DM, Dress KR, Flahive EJ, Hu Q, Kuehler JE, Kuki A, Liu W, McClellan GA, Peng Q, Plewe MB, Richardson PF, Smith GL, Solowiej J, Tran KT, Wang H, Yu X, Zhang J, Zhu H.

J Med Chem. 2011 May 12;54(9):3393-417. doi: 10.1021/jm200208d. Epub 2011 Apr 13.

PMID:
21446745
8.

Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572).

Hare S, Smith SJ, Métifiot M, Jaxa-Chamiec A, Pommier Y, Hughes SH, Cherepanov P.

Mol Pharmacol. 2011 Oct;80(4):565-72. doi: 10.1124/mol.111.073189. Epub 2011 Jun 30.

9.

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.

10.

Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.

Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ.

J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. Erratum in: J Med Chem. 2016 Jan 14;59(1):486. Childers, Karla [added]; Christensen, Melodie [added]; Kuethe, Jeffrey T. [added]; McCabe Dunn, Jamie [added]; Nolting, Andrew [added]; Peng, Zuihui [corrected].

PMID:
26397965
11.

Cross-resistance profile of the novel integrase inhibitor Dolutegravir (S/GSK1349572) using clonal viral variants selected in patients failing raltegravir.

Canducci F, Ceresola ER, Boeri E, Spagnuolo V, Cossarini F, Castagna A, Lazzarin A, Clementi M.

J Infect Dis. 2011 Dec 1;204(11):1811-5. doi: 10.1093/infdis/jir636. Epub 2011 Oct 7.

PMID:
21984737
12.

Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.

Min S, Song I, Borland J, Chen S, Lou Y, Fujiwara T, Piscitelli SC.

Antimicrob Agents Chemother. 2010 Jan;54(1):254-8. doi: 10.1128/AAC.00842-09. Epub 2009 Nov 2.

13.

Characterization of the R263K mutation in HIV-1 integrase that confers low-level resistance to the second-generation integrase strand transfer inhibitor dolutegravir.

Quashie PK, Mesplède T, Han YS, Oliveira M, Singhroy DN, Fujiwara T, Underwood MR, Wainberg MA.

J Virol. 2012 Mar;86(5):2696-705. doi: 10.1128/JVI.06591-11. Epub 2011 Dec 28.

14.

Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase.

Wang Z, Tang J, Salomon CE, Dreis CD, Vince R.

Bioorg Med Chem. 2010 Jun 15;18(12):4202-11. doi: 10.1016/j.bmc.2010.05.004. Epub 2010 May 7.

PMID:
20576573
15.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V.

J Med Chem. 2007 Oct 4;50(20):4953-75. Epub 2007 Sep 8.

PMID:
17824681
16.

S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges.

Lenz JC, Rockstroh JK.

Expert Opin Investig Drugs. 2011 Apr;20(4):537-48. doi: 10.1517/13543784.2011.562189. Epub 2011 Mar 8. Review.

PMID:
21381981
17.

Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor.

Ando M, Sato N, Nagase T, Nagai K, Ishikawa S, Takahashi H, Ohtake N, Ito J, Hirayama M, Mitobe Y, Iwaasa H, Gomori A, Matsushita H, Tadano K, Fujino N, Tanaka S, Ohe T, Ishihara A, Kanatani A, Fukami T.

Bioorg Med Chem. 2009 Aug 15;17(16):6106-22. doi: 10.1016/j.bmc.2009.05.069. Epub 2009 Jun 2.

PMID:
19616955
18.

Pharmacology of HIV integrase inhibitors.

Adams JL, Greener BN, Kashuba AD.

Curr Opin HIV AIDS. 2012 Sep;7(5):390-400. doi: 10.1097/COH.0b013e328356e91c. Review.

19.

Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.

Metobo SE, Jin H, Tsiang M, Kim CU.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3985-8. Epub 2006 May 24.

PMID:
16723226
20.

Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety.

Jin H, Metobo S, Jabri S, Mish M, Lansdown R, Chen X, Tsiang M, Wright M, Kim CU.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2263-5. doi: 10.1016/j.bmcl.2009.02.092. Epub 2009 Feb 27.

PMID:
19285389

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