Výsledky vyhledávání

Structure-Based Design of Novel Dihydroalkoxybenzyloxopyrimidine Derivatives as Potent Nonnucleoside Inhibitors of the Human Immunodeficiency Virus Reverse Transcriptase

Autor: Lisa Tuel-Ahlgren, Chen Mao, Fatih M. Uckun, Elise Sudbeck, Taracad K. Venkatachalam, Rakesh Vig

Publikováno v: Antimicrobial Agents and Chemotherapy. 42:3225-3233

Two highly potent dihydroalkoxybenzyloxopyrimidine (DABO) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of human immunodeficiency virus (HIV) reverse transcriptase (RT) have been designed based on the structure of the NNI bindi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d740299166655ed32de7bcfd9675b071
https://doi.org/10.1128/aac.42.12.3225

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Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase

Autor: Rakesh Vig, Elise A. Sudbeck, Fatih M. Uckun, Taracad K. Venkatachalam, Lisa Tuel-Ahlgren, Chen Mao

Publikováno v: Bioorganic & Medicinal Chemistry. 6:1789-1797

A series of novel phenethylthiazolylthiourea (PETT) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of HIV reverse transcriptase (RT) have been designed based on the structure of the NNI binding pocket. The structure-based design

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1866be94ef356ee36005df016f6843c2
https://doi.org/10.1016/s0968-0896(98)00108-4

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Structure-based design of N-[2-(1-piperidinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N′-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

Autor: Rakesh Vig, Taracad K. Venkatachalam, Fatih M. Uckun, Chen Mao, Elise A. Sudbeck

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:2213-2218

A novel computer model of the HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI) binding pocket, which was generated using high resolution crystal structure information from 9 individual RT/NNI complexes, revealed previously unrecognized l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::582d084e57741e6e52f25693caec4c4f
https://doi.org/10.1016/s0960-894x(98)00384-9

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5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series

Autor: Lisa Tuel-Ahlgren, Chen Mao, Taracad K. Venkatachalam, Elise A. Sudbeck, Fatih M. Uckun, Rakesh Vig

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:1461-1466

Novel dihydroalkoxybenzyloxopyrimidine (S-DABO) derivatives targeting the non-nucleoside inhibitor (NNI) binding site of human immunodeficiency virus (HIV) reverse transcriptase (RT) have been synthesized using a novel computer model for the NNI bind

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4acc2f2189fa92ff5e3e9f6b791a129b
https://doi.org/10.1016/s0960-894x(98)00250-9

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Selectin inhibition: synthesis and evaluation of novel sialylated, sulfated and fucosylated oligosaccharides, including the major capping group of GlyCAM-1

Autor: Rakesh Vig, Rakesh K. Jain, Ajit Varki, Karin E. Norgard-Sumnicht, Khushi L. Matta, Andrea Koenig

Publikováno v: Glycobiology. 7:79-93

Selectins interact with glycoconjugate ligands in important normal and pathological situations. While high affinity recognition of natural ligands is associated with alpha 1-3(4)fucosylated, alpha 2-3sialylated (and/or sulfated) lactosamine sequences

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1461d8846faa7a667e4d97557e25085f
https://doi.org/10.1093/glycob/7.1.79

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The enzymatic sulfation of glycoprotein carbohydrate units: blood group T-hapten specific and two other distinct Gal:3-O-sulfotransferases as evident from specificities and kinetics and the influence of sulfate and fucose residues occurring in the carbohydrate chain on C-3 sulfation of terminal Gal

Autor: Khushi L. Matta, Rakesh K. Jain, Rakesh Vig, E. V. Chandrasekaran

Publikováno v: Glycobiology. 7:753-767

Enzymatic 3-O-sulfation of terminal beta-Gal residues was investigated by screening sulfotransferase activity present in 37 human tissue specimens toward the following synthesized acceptor moieties: Galbeta1,3GalNAc alpha-O-Al, Galbeta1,4GlcNAcbeta-O

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5335195c996aaeb3e619afca23852581
https://doi.org/10.1093/glycob/7.6.753

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Nucleoside Conjugates. 15. Synthesis and Biological Activity of Anti-HIV Nucleoside Conjugates of Ether and Thioether Phospholipids

Autor: Chung K. Chu, Konstantine K. Manouilov, Alexander Nechaev, Charles R. West, Alan J. Kirisits, Chung I. Hong, Rakesh Vig

Publikováno v: Journal of Medicinal Chemistry. 39:1771-1777

A series of the anti-HIV nucleoside conjugates of either (1-O-alkyl) and thioether (1-S-alkyl) lipids linked by a pyrophosphate diester bond has been synthesized as micelle-forming prodrugs of the nucleosides to improve their therapeutic efficiency.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fea4a74469506843e7c8165fe4831a64
https://doi.org/10.1021/jm950620o

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Synthesis and antitumor activity of 1-β-D-arabinofuranosylcytosine conjugates of optical isomers of ether and thioether lipids

Autor: Charles R. West, Rakesh Vig, Alan J. Kirisits, Seung-Ho An, Alexander Nechaev, Chung Hong

Publikováno v: Lipids. 28:1021-1026

Four 1-beta-D-arabinofuranosylcytosine conjugates (ara-C) (1a, b and 2a, b) of sn-1 and sn-3 isomers of 1-O-octadecyl-2-O-palmitoylglycerol and its 1-S-alkyl analogue have been synthesized, and their antitumor activity against L1210 lymphoid leukemia

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2adadc0ff78a37b67cfc2503429875d
https://doi.org/10.1007/bf02537125

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