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Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043).

Kadow JF, Ueda Y, Meanwell NA, Connolly TP, Wang T, Chen CP, Yeung KS, Zhu J, Bender JA, Yang Z, Parker D, Lin PF, Colonno RJ, Mathew M, Morgan D, Zheng M, Chien C, Grasela D.

J Med Chem. 2012 Mar 8;55(5):2048-56. doi: 10.1021/jm201218m. Epub 2012 Feb 22.


Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity in HIV-1-infected subjects.

Wang T, Yin Z, Zhang Z, Bender JA, Yang Z, Johnson G, Yang Z, Zadjura LM, D'Arienzo CJ, DiGiugno Parker D, Gesenberg C, Yamanaka GA, Gong YF, Ho HT, Fang H, Zhou N, McAuliffe BV, Eggers BJ, Fan L, Nowicka-Sans B, Dicker IB, Gao Q, Colonno RJ, Lin PF, Meanwell NA, Kadow JF.

J Med Chem. 2009 Dec 10;52(23):7778-87. doi: 10.1021/jm900843g.


Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248.

Regueiro-Ren A, Simmermacher-Mayer J, Sinz M, Johnson KA, Huang XS, Jenkins S, Parker D, Rahematpura S, Zheng M, Meanwell NA, Kadow JF.

J Med Chem. 2013 Feb 28;56(4):1670-6. doi: 10.1021/jm301638a. Epub 2013 Feb 12.


Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions.

Wang T, Zhang Z, Wallace OB, Deshpande M, Fang H, Yang Z, Zadjura LM, Tweedie DL, Huang S, Zhao F, Ranadive S, Robinson BS, Gong YF, Ricarrdi K, Spicer TP, Deminie C, Rose R, Wang HG, Blair WS, Shi PY, Lin PF, Colonno RJ, Meanwell NA.

J Med Chem. 2003 Sep 25;46(20):4236-9.


Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-585248).

Regueiro-Ren A, Xue QM, Swidorski JJ, Gong YF, Mathew M, Parker DD, Yang Z, Eggers B, D'Arienzo C, Sun Y, Malinowski J, Gao Q, Wu D, Langley DR, Colonno RJ, Chien C, Grasela DM, Zheng M, Lin PF, Meanwell NA, Kadow JF.

J Med Chem. 2013 Feb 28;56(4):1656-69. doi: 10.1021/jm3016377. Epub 2013 Feb 7.


Inhibitors of HIV-1 attachment. Part 9: an assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative.

Yeung KS, Qiu Z, Yang Z, Zadjura L, D'Arienzo CJ, Browning MR, Hansel S, Huang XS, Eggers BJ, Riccardi K, Lin PF, Meanwell NA, Kadow JF.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):209-12. doi: 10.1016/j.bmcl.2012.10.125. Epub 2012 Nov 7.


Preclinical pharmacokinetics of a novel HIV-1 attachment inhibitor BMS-378806 and prediction of its human pharmacokinetics.

Yang Z, Zadjura L, D'Arienzo C, Marino A, Santone K, Klunk L, Greene D, Lin PF, Colonno R, Wang T, Meanwell N, Hansel S.

Biopharm Drug Dispos. 2005 Dec;26(9):387-402.


Inhibitors of HIV-1 attachment. Part 10. The discovery and structure-activity relationships of 4-azaindole cores.

Wang T, Yang Z, Zhang Z, Gong YF, Riccardi KA, Lin PF, Parker DD, Rahematpura S, Mathew M, Zheng M, Meanwell NA, Kadow JF, Bender JA.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):213-7. doi: 10.1016/j.bmcl.2012.10.120. Epub 2012 Nov 7.


Inhibitors of HIV-1 attachment. Part 11: the discovery and structure-activity relationships associated with 4,6-diazaindole cores.

Bender JA, Yang Z, Eggers B, Gong YF, Lin PF, Parker DD, Rahematpura S, Zheng M, Meanwell NA, Kadow JF.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):218-22. doi: 10.1016/j.bmcl.2012.10.118. Epub 2012 Nov 5.


Compartmental absorption modeling and site of absorption studies to determine feasibility of an extended-release formulation of an HIV-1 attachment inhibitor phosphate ester prodrug.

Brown J, Chien C, Timmins P, Dennis A, Doll W, Sandefer E, Page R, Nettles RE, Zhu L, Grasela D.

J Pharm Sci. 2013 Jun;102(6):1742-51. doi: 10.1002/jps.23476. Epub 2013 Apr 5.


5'-phosphonate derivatives of 2',3'-dideoxy-3'-thiacytidine as new anti-HIV prodrugs.

Khandazhinskaya AL, Jasko MV, Karpenko IL, Solyev PN, Golubeva NA, Kukhanova MK.

Chem Biol Drug Des. 2011 Jul;78(1):50-6. doi: 10.1111/j.1747-0285.2011.01129.x. Epub 2011 May 31.


Utilization of in vitro Caco-2 permeability and liver microsomal half-life screens in discovering BMS-488043, a novel HIV-1 attachment inhibitor with improved pharmacokinetic properties.

Yang Z, Zadjura LM, Marino AM, D'Arienzo CJ, Malinowski J, Gesenberg C, Lin PF, Colonno RJ, Wang T, Kadow JF, Meanwell NA, Hansel SB.

J Pharm Sci. 2010 Apr;99(4):2135-52. doi: 10.1002/jps.21948.


Novel approaches for designing 5'-O-ester prodrugs of 3'-azido-2', 3'-dideoxythymidine (AZT).

Parang K, Wiebe LI, Knaus EE.

Curr Med Chem. 2000 Oct;7(10):995-1039. Review.


Frequency of amino acid changes associated with resistance to attachment inhibitor BMS-626529 in R5- and X4-tropic HIV-1 subtype B.

SouliƩ C, Lambert-Niclot S, Fofana DB, Fourati S, Ait-Arkoub Z, Sayon S, Simon A, Katlama C, Calvez V, Marcelin AG.

J Antimicrob Chemother. 2013 Jun;68(6):1243-5. doi: 10.1093/jac/dkt018. Epub 2013 Feb 8.


Genotypic correlates of susceptibility to HIV-1 attachment inhibitor BMS-626529, the active agent of the prodrug BMS-663068.

Zhou N, Nowicka-Sans B, McAuliffe B, Ray N, Eggers B, Fang H, Fan L, Healy M, Langley DR, Hwang C, Lataillade M, Hanna GJ, Krystal M.

J Antimicrob Chemother. 2014 Mar;69(3):573-81. doi: 10.1093/jac/dkt412. Epub 2013 Oct 14.


Inhibitors of HIV-1 attachment. Part 4: A study of the effect of piperazine substitution patterns on antiviral potency in the context of indole-based derivatives.

Wang T, Kadow JF, Zhang Z, Yin Z, Gao Q, Wu D, Parker DD, Yang Z, Zadjura L, Robinson BA, Gong YF, Spicer TP, Blair WS, Shi PY, Yamanaka G, Lin PF, Meanwell NA.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5140-5. doi: 10.1016/j.bmcl.2009.07.076. Epub 2009 Jul 18. Erratum in: Bioorg Med Chem Lett. 2010 Feb 15;20(4):1462. Spicer, Timothy P [added].


A prodrug approach toward the development of water soluble fluoroquinolones and structure--activity relationships of quinoline-3-carboxylic acids.

Baker WR, Cai S, Dimitroff M, Fang L, Huh KK, Ryckman DR, Shang X, Shawar RM, Therrien JH.

J Med Chem. 2004 Sep 9;47(19):4693-709.


Enhancement of oral bioavailability of an HIV-attachment inhibitor by nanosizing and amorphous formulation approaches.

Fakes MG, Vakkalagadda BJ, Qian F, Desikan S, Gandhi RB, Lai C, Hsieh A, Franchini MK, Toale H, Brown J.

Int J Pharm. 2009 Mar 31;370(1-2):167-74. doi: 10.1016/j.ijpharm.2008.11.018. Epub 2008 Nov 28.


Synthesis of the 6-azaindole containing HIV-1 attachment inhibitor pro-drug, BMS-663068.

Chen K, Risatti C, Bultman M, Soumeillant M, Simpson J, Zheng B, Fanfair D, Mahoney M, Mudryk B, Fox RJ, Hsaio Y, Murugesan S, Conlon DA, Buono FG, Eastgate MD.

J Org Chem. 2014 Sep 19;79(18):8757-67. doi: 10.1021/jo5016008. Epub 2014 Sep 5.


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