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Results: 1 to 20 of 102

1.

Nucleotide competing reverse transcriptase inhibitors: discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.

James CA, DeRoy P, Duplessis M, Edwards PJ, Halmos T, Minville J, Morency L, Morin S, Simoneau B, Tremblay M, Bethell R, Cordingley M, Duan J, Lamorte L, Pelletier A, Rajotte D, Salois P, Tremblay S, Sturino CF.

Bioorg Med Chem Lett. 2013 May 1;23(9):2781-6. doi: 10.1016/j.bmcl.2013.02.021. Epub 2013 Feb 13.

PMID:
23545107
[PubMed - indexed for MEDLINE]
2.

Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors.

Tremblay M, Bethell RC, Cordingley MG, DeRoy P, Duan J, Duplessis M, Edwards PJ, Faucher AM, Halmos T, James CA, Kuhn C, Lacoste JÉ, Lamorte L, LaPlante SR, Malenfant E, Minville J, Morency L, Morin S, Rajotte D, Salois P, Simoneau B, Tremblay S, Sturino CF.

Bioorg Med Chem Lett. 2013 May 1;23(9):2775-80. doi: 10.1016/j.bmcl.2013.02.042. Epub 2013 Feb 16.

PMID:
23511023
[PubMed - indexed for MEDLINE]
3.

Identification of potent and orally bioavailable nucleotide competing reverse transcriptase inhibitors: in vitro and in vivo optimization of a series of benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.

Sturino CF, Bousquet Y, James CA, DeRoy P, Duplessis M, Edwards PJ, Halmos T, Minville J, Morency L, Morin S, Thavonekham B, Tremblay M, Duan J, Ribadeneira M, Garneau M, Pelletier A, Tremblay S, Lamorte L, Bethell R, Cordingley MG, Rajotte D, Simoneau B.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3967-75. doi: 10.1016/j.bmcl.2013.04.043. Epub 2013 Apr 25.

PMID:
23673016
[PubMed - indexed for MEDLINE]
4.

Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor series.

Rajotte D, Tremblay S, Pelletier A, Salois P, Bourgon L, Coulombe R, Mason S, Lamorte L, Sturino CF, Bethell R.

Antimicrob Agents Chemother. 2013 Jun;57(6):2712-8. doi: 10.1128/AAC.00113-13. Epub 2013 Apr 1.

PMID:
23545531
[PubMed - indexed for MEDLINE]
Free PMC Article
5.

Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Zhang J, Zhan P, Wu J, Li Z, Jiang Y, Ge W, Pannecouque C, De Clercq E, Liu X.

Bioorg Med Chem. 2011 Jul 15;19(14):4366-76. doi: 10.1016/j.bmc.2011.05.024. Epub 2011 May 23.

PMID:
21683601
[PubMed - indexed for MEDLINE]
6.

A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability.

Kim J, Ok T, Park C, So W, Jo M, Kim Y, Seo M, Lee D, Jo S, Ko Y, Choi I, Park Y, Yoon J, Ju MK, Ahn J, Kim J, Han SJ, Kim TH, Cechetto J, Nam J, Liuzzi M, Sommer P, No Z.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2522-6. doi: 10.1016/j.bmcl.2012.01.133. Epub 2012 Feb 8.

PMID:
22374216
[PubMed - indexed for MEDLINE]
7.

N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Mitchell ML, Son JC, Lee IY, Lee CK, Kim HS, Guo H, Wang J, Hayes J, Wang M, Paul A, Lansdon EB, Chen JM, Eisenberg G, Geleziunas R, Xu L, Kim CU.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1585-8. doi: 10.1016/j.bmcl.2010.01.086. Epub 2010 Jan 21.

PMID:
20137928
[PubMed - indexed for MEDLINE]
8.

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Mai A, Sbardella G, Artico M, Ragno R, Massa S, Novellino E, Greco G, Lavecchia A, Musiu C, La Colla M, Murgioni C, La Colla P, Loddo R.

J Med Chem. 2001 Aug 2;44(16):2544-54.

PMID:
11472208
[PubMed - indexed for MEDLINE]
9.

Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.

Wang YP, Chen FE, De Clercq E, Balzarini J, Pannecouque C.

Eur J Med Chem. 2009 Mar;44(3):1016-23. doi: 10.1016/j.ejmech.2008.06.028. Epub 2008 Jul 4.

PMID:
18692274
[PubMed - indexed for MEDLINE]
10.

Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.

Wu HQ, Yan ZH, Chen WX, He QQ, Chen FE, De Clercq E, Balzarini J, Daelemans D, Pannecouque C.

Bioorg Med Chem. 2013 Nov 1;21(21):6477-83. doi: 10.1016/j.bmc.2013.08.040. Epub 2013 Aug 30.

PMID:
24055077
[PubMed - indexed for MEDLINE]
11.

Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.

Rotili D, Tarantino D, Nawrozkij MB, Babushkin AS, Botta G, Marrocco B, Cirilli R, Menta S, Badia R, Crespan E, Ballante F, Ragno R, Esté JA, Maga G, Mai A.

J Med Chem. 2014 Jun 26;57(12):5212-25. doi: 10.1021/jm500284x. Epub 2014 Jun 16.

PMID:
24933420
[PubMed - indexed for MEDLINE]
12.

Structure-based design of novel dihydroalkoxybenzyloxopyrimidine derivatives as potent nonnucleoside inhibitors of the human immunodeficiency virus reverse transcriptase.

Sudbeck EA, Mao C, Vig R, Venkatachalam TK, Tuel-Ahlgren L, Uckun FM.

Antimicrob Agents Chemother. 1998 Dec;42(12):3225-33.

PMID:
9835518
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Mitchell ML, Son JC, Guo H, Im YA, Cho EJ, Wang J, Hayes J, Wang M, Paul A, Lansdon EB, Chen JM, Graupe D, Rhodes G, He GX, Geleziunas R, Xu L, Kim CU.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1589-92. doi: 10.1016/j.bmcl.2010.01.085. Epub 2010 Jan 21.

PMID:
20138513
[PubMed - indexed for MEDLINE]
14.

Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.

Ragno R, Mai A, Sbardella G, Artico M, Massa S, Musiu C, Mura M, Marturana F, Cadeddu A, La Colla P.

J Med Chem. 2004 Feb 12;47(4):928-34.

PMID:
14761194
[PubMed - indexed for MEDLINE]
15.

Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Ji L, Chen FE, De Clercq E, Balzarini J, Pannecouque C.

J Med Chem. 2007 Apr 19;50(8):1778-86. Epub 2007 Mar 24. Erratum in: J Med Chem. 2007 Jun 14;50(12):2930.

PMID:
17381078
[PubMed - indexed for MEDLINE]
16.

Nonnucleoside HIV-1 reverse transcriptase inhibitors; part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxyl-carbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones.

He Y, Chen F, Yu X, Wang Y, De Clercq E, Balzarini J, Pannecouque C.

Bioorg Chem. 2004 Dec;32(6):536-48.

PMID:
15530994
[PubMed - indexed for MEDLINE]
17.

Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

Tucker TJ, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Reid JC, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y.

J Med Chem. 2008 Oct 23;51(20):6503-11. doi: 10.1021/jm800856c. Epub 2008 Oct 1.

PMID:
18826204
[PubMed - indexed for MEDLINE]
18.

Synthesis and biological evaluation of 6-substituted 5-alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.

Yu M, Li Z, Liu S, Fan E, Pannecouque C, De Clercq E, Liu X.

ChemMedChem. 2011 May 2;6(5):826-33. doi: 10.1002/cmdc.201000555. Epub 2011 Feb 14.

PMID:
21322110
[PubMed - indexed for MEDLINE]
19.

The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4-dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro.

Long J, Zhang DH, Zhang GH, Rao ZK, Wang YH, Tam SC, He YP, Zheng YT.

Yao Xue Xue Bao. 2010 Feb;45(2):228-34.

PMID:
21348416
[PubMed - indexed for MEDLINE]
20.

Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.

Qin H, Liu C, Guo Y, Wang R, Zhang J, Ma L, Zhang Z, Wang X, Cui Y, Liu J.

Bioorg Med Chem. 2010 May 1;18(9):3231-7. doi: 10.1016/j.bmc.2010.03.025. Epub 2010 Mar 15.

PMID:
20371182
[PubMed - indexed for MEDLINE]

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