Search Results - "Yudkovitz, Joel B"

Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists by Simeone, Joseph P, Bugianesi, Robert L, Ponpipom, Mitree M, Yang, Yi Tien, Lo, Jane-Ling, Yudkovitz, Joel B, Cui, Jisong, Mount, George R, Ren, Rena Ning, Creighton, Mellissa, Mao, An-Hua, Vincent, Stella H, Cheng, Kang, Goulet, Mark T

“…The synthesis of a number of indole GnRH antagonists is described. Oxidation of the pyridine ring nitrogen, combined with alkylation at the two position, led…”
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Syntheses and structure–activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists by Jiang, Jinlong, DeVita, Robert J., Goulet, Mark T., Wyvratt, Matthew J., Lo, Jane-L., Ren, Ning, Yudkovitz, Joel B., Cui, Jisong, Yang, Yi T., Cheng, Kang, Rohrer, Susan P.

“…Syntheses and structure–activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described…”
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A Potent, Nonpeptidyl 1H-Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor by DeVita, Robert J, Walsh, Thomas F, Young, Jonathan R, Jiang, Jinlong, Ujjainwalla, Feroze, Toupence, Richard B, Parikh, Mamta, Huang, Song X, Fair, Jason A, Goulet, Mark T, Wyvratt, Matthew J, Lo, Jane-L, Ren, Ning, Yudkovitz, Joel B, Yang, Yi T, Cheng, Kang, Cui, Jisong, Mount, George, Rohrer, Susan P, Schaeffer, James M, Rhodes, Linda, Drisko, Jennifer E, McGowan, Erin, MacIntyre, D. Euan, Vincent, Styliani, Carlin, Josephine R, Cameron, Judith, Smith, Roy G

“…Extensive development of the structure−activity relationships of a screening lead determined three important pharmacophores for gonadotropin-releasing hormone…”
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Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity by Ashton, Wallace T., Sisco, Rosemary M., Kieczykowski, Gerard R., Yang, Yi Tien, Yudkovitz, Joel B., Cui, Jisong, Mount, George R., Ren, Rena Ning, Wu, Tsuei-Ju, Shen, Xiaolan, Lyons, Kathryn A., Mao, An-Hua, Carlin, Josephine R., Karanam, Bindhu V., Vincent, Stella H., Cheng, Kang, Goulet, Mark T.

“…Stereospecific introduction of a methyl group to the indole-3-side chain enhanced activity in our tryptamine-derived series of GnRH receptor antagonists…”
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Substituted Indole-5-carboxamides and -acetamides as Potent Nonpeptide GnRH Receptor Antagonists by Ashton, Wallace T., Sisco, Rosemary M., Yang, Yi Tien, Lo, Jane-Ling, Yudkovitz, Joel B., Cheng, Kang, Goulet, Mark T.

“…The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With…”
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2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain by Young, Jonathan R., Huang, Song X., Walsh, Thomas F., Wyvratt, Matthew J., Yang, Yi Tien, Yudkovitz, Joel B., Cui, Jisong, Mount, George R., Ren, Rena Ning, Wu, Tsuei-Ju, Shen, Xiaolan, Lyons, Kathryn A., Mao, An-Hua, Carlin, Josephine R., Karanam, Bindhu V., Vincent, Stella H., Cheng, Kang, Goulet, Mark T.

“…A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their…”
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Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus by Ashton, Wallace T., Sisco, Rosemary M., Yang, Yi Tien, Lo, Jane-Ling, Yudkovitz, Joel B., Gibbons, Patrice H., Mount, George R., Ren, Rena Ning, Butler, Bridget S., Cheng, Kang, Goulet, Mark T.

“…A pyridine side-chain terminus has been incorporated into the indole-5-carboxamide and indole-5-acetamide series of GnRH antagonists. Potent activity was…”
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Identification of neutral 4- O-alkyl quinolone nonpeptide GnRH receptor antagonists by DeVita, Robert J., Parikh, Mamta, Jiang, Jinlong, Fair, Jason A., Young, Jonathan R., Walsh, Thomas F., Goulet, Mark T., Lo, Jane-L., Ren, Ning, Yudkovitz, Joel B., Cui, Jisong, Yang, Yi T., Cheng, Kang, Rohrer, Susan P., Wyvratt, Matthew J.

“…Potent neutral replacements of the basic amine at the 4-position of quinolone non-peptide GnRH antagonists are reported. A series of neutral, nonbasic…”
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Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides by Walsh, Thomas F, Toupence, Richard B, Young, Jonathan R, Huang, Song X, Ujjainwalla, Feroze, DeVita, Robert J, Goulet, Mark T, Wyvratt, Matthew J, Fisher, Michael H, Lo, Jane-Ling, Ren, Ning, Yudkovitz, Joel B, Yang, Yi Tien, Cheng, Kang, Smith, Roy G

“…SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic…”
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Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents by Young, Jonathan R., Huang, Song X., Chen, Irene, Walsh, Thomas F., DeVita, Robert J., Wyvratt, Matthew J., Goulet, Mark T., Ren, Ning, Lo, Jane, Yang, Yi Tien, Yudkovitz, Joel B., Cheng, Kang, Smith, Roy G.

“…A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of…”
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A Potent, Nonpeptidyl 1 H -Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor by DeVita, Robert J., Walsh, Thomas F., Young, Jonathan R., Jiang, Jinlong, Ujjainwalla, Feroze, Toupence, Richard B., Parikh, Mamta, Huang, Song X., Fair, Jason A., Goulet, Mark T., Wyvratt, Matthew J., Lo, Jane-L., Ren, Ning, Yudkovitz, Joel B., Yang, Yi T., Cheng, Kang, Cui, Jisong, Mount, George, Rohrer, Susan P., Schaeffer, James M., Rhodes, Linda, Drisko, Jennifer E., McGowan, Erin, MacIntyre, D. Euan, Vincent, Styliani, Carlin, Josephine R., Cameron, Judith, Smith, Roy G.

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Inhibition of Hydroxymethylglutaryl-Coenzyme A Synthase by L-659,699 by Greenspan, Michael D., Yudkovitz, Joel B., Lo, Chia-Yee L., Chen, Julie S., Alberts, Alfred W., Hunt, Vincent M., Chang, Michael N., Yang, Shu Shu, Thompson, Kathryn L., Chiang, Yuan-Ching P., Chabala, John C., Monaghan, Richard L., Schwartz, Robert L.

“…A β -lactone isolated from Fusarium sp. has been shown to be a potent specific inhibitor of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase…”
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The inhibition of cytoplasmic acetoacetyl-CoA thiolase by a triyne carbonate (L-660, 631) by Greenspan, M D, Yudkovitz, J B, Chen, J S, Hanf, D P, Chang, M N, Chiang, P Y, Chabala, J C, Alberts, A W

“…The compound L-660, 631 (2-oxo-5-(1-hydroxy-2,4,6-heptatriynyl)-1,3-dioxolane-4 heptanoic acid), a natural product isolated from an Actinomycete culture, was…”
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A sensitive assay for phosphatidate phosphohydrolase in mouse liver microsomes by Germershausen, J I, Yudkovitz, J B, Greenspan, M D

“…A technique is described for the assay of phosphatidate phosphohydrolase using 1,2-[9,10-3H]dioleoyl-sn-glycero-3-phosphate as a substrate. This substrate was…”
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