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Items: 1 to 20 of 99

1.

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.

PMID:
23200244
2.

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.

PMID:
23374053
3.

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.

PMID:
22356441
4.

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.

PMID:
23200254
5.

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.

PMID:
23206859
6.

Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors.

Yeung KS, Qiu Z, Yin Z, Trehan A, Fang H, Pearce B, Yang Z, Zadjura L, D'Arienzo CJ, Riccardi K, Shi PY, Spicer TP, Gong YF, Browning MR, Hansel S, Santone K, Barker J, Coulter T, Lin PF, Meanwell NA, Kadow JF.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):203-8. doi: 10.1016/j.bmcl.2012.10.117. Epub 2012 Nov 5.

PMID:
23200249
7.

Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents.

Yeung KS, Qiu Z, Xue Q, Fang H, Yang Z, Zadjura L, D'Arienzo CJ, Eggers BJ, Riccardi K, Shi PY, Gong YF, Browning MR, Gao Q, Hansel S, Santone K, Lin PF, Meanwell NA, Kadow JF.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):198-202. doi: 10.1016/j.bmcl.2012.10.115. Epub 2012 Nov 6.

PMID:
23200252
8.

Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of potential prodrugs of benzimidazole-7-carboxylic acids.

Kubo K, Kohara Y, Yoshimura Y, Inada Y, Shibouta Y, Furukawa Y, Kato T, Nishikawa K, Naka T.

J Med Chem. 1993 Aug 6;36(16):2343-9.

PMID:
8360879
9.

Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation.

Park JH, Chang JS, El-Gamal MI, Choi WK, Lee WS, Chung HJ, Kim HI, Cho YJ, Lee BS, Jeon HR, Lee YS, Choi YW, Lee J, Oh CH.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5895-9. doi: 10.1016/j.bmcl.2010.07.089. Epub 2010 Jul 25.

PMID:
20728357
10.

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.

PMID:
10911016
11.
12.

Prodrugs to improve the oral bioavailability of a diacidic nonpeptide angiotensin II antagonist.

Aungst BJ, Blake JA, Rogers NJ, Saitoh H, Hussain MA, Ensinger CL, Pruitt JR.

Pharm Res. 1995 May;12(5):763-7.

PMID:
7479565
13.

Inhibitors of acyl-CoA:cholesterol O-acyltransferase. synthesis and pharmacological activity of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide and structurally related tetrazole amide derivatives.

O'Brien PM, Sliskovic DR, Picard JA, Lee HT, Purchase CF 2nd, Roth BD, White AD, Anderson M, Mueller SB, Bocan T, Bousley R, Hamelehle KL, Homan R, Lee P, Krause BR, Reindel JF, Stanfield RL, Turluck D.

J Med Chem. 1996 Jun 7;39(12):2354-66.

PMID:
8691430
14.

Metabolism and pharmacokinetics of novel oral prodrugs of 9-[(R)-2-(phosphonomethoxy)propyl]adenine (PMPA) in dogs.

Shaw JP, Sueoko CM, Oliyai R, Lee WA, Arimilli MN, Kim CU, Cundy KC.

Pharm Res. 1997 Dec;14(12):1824-9.

PMID:
9453075
15.

Cardiotonic agents. 7. Prodrug derivatives of 4-ethyl-1,3-dihydro- 5-[4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H-imidazol-2-one.

Shaw KJ, Erhardt PW, Hagedorn AA 3rd, Pease CA, Ingebretsen WR, Wiggins JR.

J Med Chem. 1992 Apr 3;35(7):1267-72.

PMID:
1560439
16.

Synthesis of poly(ethylene glycol)-based saquinavir prodrug conjugates and assessment of release and anti-HIV-1 bioactivity using a novel protease inhibition assay.

Gunaseelan S, Debrah O, Wan L, Leibowitz MJ, Rabson AB, Stein S, Sinko PJ.

Bioconjug Chem. 2004 Nov-Dec;15(6):1322-33.

PMID:
15546199
17.

Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.

Gagnon A, Landry S, Coulombe R, Jakalian A, Guse I, Thavonekham B, Bonneau PR, Yoakim C, Simoneau B.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1199-205. doi: 10.1016/j.bmcl.2008.12.074. Epub 2008 Dec 24.

PMID:
19138518
18.

New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation.

Vlieghe P, Bihel F, Clerc T, Pannecouque C, Witvrouw M, De Clercq E, Salles JP, Chermann JC, Kraus JL.

J Med Chem. 2001 Mar 1;44(5):777-86.

PMID:
11262088
20.

Prodrugs of HIV protease inhibitors-saquinavir, indinavir and nelfinavir-derived from diglycerides or amino acids: synthesis, stability and anti-HIV activity.

Gaucher B, Rouquayrol M, Roche D, Greiner J, Aubertin AM, Vierling P.

Org Biomol Chem. 2004 Feb 7;2(3):345-57. Epub 2004 Jan 5.

PMID:
14747863
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