Search Results - "Bindhu V. Karanam"

Antidiabetic and antisteatotic effects of the selective fatty acid synthase (FAS) inhibitor platensimycin in mouse models of diabetes by Wu, Margaret, Singh, Sheo B, Wang, Jun, Chung, Christine C, Salituro, Gino, Karanam, Bindhu V, Lee, Sang Ho, Powles, Maryann, Ellsworth, Kenneth P, Lassman, Michael E, Miller, Corey, Myers, Robert W, Tota, Michael R, Zhang, Bei B, Li, Cai

“…Platensimycin (PTM) is a recently discovered broad-spectrum antibiotic produced by Streptomyces platensis. It acts by selectively inhibiting the…”
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Identification and characterization of sebaceous gland atrophy-sparing DGAT1 inhibitors by Muise, Eric S, Zhu, Yonghua, Verras, Andreas, Karanam, Bindhu V, Gorski, Judith, Weingarth, Drew, Lin, Hua V, Hwa, Joyce, Thompson, John R, Hu, Guanghui, Liu, Jian, He, Shuwen, DeVita, Robert J, Shen, Dong-Ming, Pinto, Shirly

“…Inhibition of Diacylglycerol O-acyltransferase 1 (DGAT1) has been a mechanism of interest for metabolic disorders. DGAT1 inhibition has been shown to be a key…”
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Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes by Shah, Shrenik K, He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yang, Wong, Frederick, Samuel, Koppara, Madiera, Maria, Karanam, Bindhu V, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Feng, Yue, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Eiermann, George J, Li, Cai, Pachanski, Michele, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Morissette, Pierre, Volksdorf, Sylvia, Kerr, Janet, Zhang, Bei B, Howard, Andrew D, Zhou, Yun-Ping, Pasternak, Alexander, Nargund, Ravi P, Hagmann, William K

“…The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a…”
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Mechanistic Studies on the Metabolic Scission of Thiazolidinedione Derivatives to Acyclic Thiols by Reddy, Vijay Bhasker G, Karanam, Bindhu V, Gruber, Wendy L, Wallace, Michael A, Vincent, Stella H, Franklin, Ronald B, Baillie, Thomas A

“…Thiazolidinedione (TZD) derivatives have been reported to undergo metabolic activation of the TZD ring to produce reactive intermediates. In the case of…”
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SPECIES DIFFERENTIAL STEREOSELECTIVE OXIDATION OF A METHYLSULFIDE METABOLITE OF MK-0767 [(±)-5-[(2,4-DIOXOTHIAZOLIDIN-5-YL)METHYL]-2-METHOXY-N-[[(4-TRIFLUOROMETHYL)PHENYL]METHYL]BENZAMIDE], A PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR DUAL AGONIST by KARANAM, Bindhu V, WELCH, Christopher J, REDDY, Vijay G, CHILENSKI, Jennifer, BIBA, Mirlinda, VINCENT, Stella

“…MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy- N -[[(4-trifluoromethyl)phenyl]methyl]benzamide], a thiazolidinedione (TZD)-containing…”
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Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC) by Yu, Yang, Wu, Zhicai, Shi, Zhi-Cai, He, Shuwen, Lai, Zhong, Cernak, Timothy A., Vachal, Petr, Liu, Min, Liu, Jian, Hong, Qingmei, Jian, Tianying, Guiadeen, Deodial, Krikorian, Arto, Sperbeck, Donald M., Verras, Andreas, Sonatore, Lisa M., Murphy, Beth A., Wiltsie, Judyann, Chung, Christine C., Gorski, Judith N., Liu, Jinqi, Xiao, Jianying, Wolff, Michael, Tong, Sharon X., Madeira, Maria, Karanam, Bindhu V., Shen, Dong-Ming, Balkovec, James M., De Vita, Robert J., Pinto, Shirly, Nargund, Ravi P.

“…[Display omitted] The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1)…”
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Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety by He, Shuwen, Lai, Zhong, Hong, Qingmei, Shang, Jackie, Reibarkh, Mikhail, Kuethe, Jeffrey T., Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D., Cernak, Timothy A., Dykstra, Kevin D., Sperbeck, Donald M., Wu, Zhicai, Yu, Yang, Yang, Ginger X., Jian, Tianying, Verras, Andreas, Sonatore, Lisa M., Wiltsie, Judyann, Chung, Christine C., Murphy, Beth A., Gorski, Judith N., Liu, Jinqi, Xiao, Jianying, Wolff, Michael, Tong, Sharon X., Madeira, Maria, Karanam, Bindhu V., Shen, Dong-Ming, Balkovec, James M., Pinto, Shirly, Nargund, Ravi P., DeVita, Robert J.

“…Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of…”
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IDENTIFICATION AND METABOLISM OF A NOVEL DIHYDROHYDROXY-S-GLUTATHIONYL CONJUGATE OF A PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR AGONIST, MK-0767 [(±)-5-[(2,4-DIOXOTHIAZOLIDIN-5-YL)METHYL]-2-METHOXY-N-[[(4-TRIFLUOROMETHYL) PHENYL]METHYL]BENZAMIDE], IN RATS by REDDY, Vijay Bhasker G, DOSS, George A, CREIGHTON, Mellissa, KOCHANSKY, Christopher J, VINCENT, Stella H, FRANKLIN, Ronald B, KARANAM, Bindhu V

“…MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy- N -[[(4-trifluoromethyl)phenyl]methyl]benzamide] is a novel thiazolidinedione-containing…”
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A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain by Hoyt, Scott B., London, Clare, Abbadie, Catherine, Felix, John P., Garcia, Maria L., Jochnowitz, Nina, Karanam, Bindhu V., Li, Xiaohua, Lyons, Kathryn A., McGowan, Erin, Priest, Birgit T., Smith, McHardy M., Warren, Vivien A., Thomas-Fowlkes, Brande S., Kaczorowski, Gregory J., Duffy, Joseph L.

“…A series of benzazepinones were synthesized and evaluated as Nav1.7 sodium channel blockers. Compound 30 from this series displayed potent channel block, good…”
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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety by He, Shuwen, Hong, Qingmei, Lai, Zhong, Yang, David X, Ting, Pauline C, Kuethe, Jeffrey T, Cernak, Timothy A, Dykstra, Kevin D, Sperbeck, Donald M, Wu, Zhicai, Yu, Yang, Yang, Ginger X, Jian, Tianying, Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D, Sonatore, Lisa M, Wiltsie, Judyann, Liu, Jinqi, Gorski, Judith N, Chung, Christine C, Gibson, Jack T, Lisnock, JeanMarie, Xiao, Jianying, Wolff, Michael, Tong, Sharon X, Madeira, Maria, Karanam, Bindhu V, Shen, Dong-Ming, Balkovec, James M, Pinto, Shirly, Nargund, Ravi P, DeVita, Robert J

“…We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel…”
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Benzazepinone Nav1.7 blockers : Potential treatments for neuropathic pain by HOYT, Scott B, LONDON, Clare, KARANAM, Bindhu V, XIAOHUA LI, LYONS, Kathryn A, MCGOWAN, Erin, EUAN MACINTYRE, D, MARTIN, William J, PRIEST, Birgit T, SMITH, Mchardy M, TSCHIRRET-GUTH, Richard, WARREN, Vivien A, OK, Hyun, WILLIAMS, Brande S, KACZOROWSKI, Gregory J, PARSONS, William H, GONZALEZ, Edward, DUFFY, Joseph L, ABBADIE, Catherine, DEAN, Brian, FELIX, John P, GARCIA, Maria L, JOCHNOWITZ, Nina

“…A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral…”
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Imidazopyridines : A novel class of hNav1.7 channel blockers by LONDON, Clare, HOYT, Scott B, LYONS, Kathryn A, XIAOHUA LI, KARANAM, Bindhu V, JOCHNOWITZ, Nina, GARCIA, Maria L, FELIX, John P, DEAN, Brian, ABBADIE, Catherine, KACZOROWSKI, Gregory J, DUFFY, Joseph L, PARSONS, William H, WILLIAMS, Brande S, WARREN, Vivien A, TSCHIRRET-GUTH, Richard, SMITH, Mchardy M, PRIEST, Birgit T, MCGOWAN, Erin, MARTIN, William J

“…A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with…”
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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety by He, Shuwen, Hong, Qingmei, Lai, Zhong, Wu, Zhicai, Yu, Yang, Kim, David W, Ting, Pauline C, Kuethe, Jeffrey T, Yang, Ginger X, Jian, Tianying, Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D, Sperbeck, Donald M, Sonatore, Lisa M, Wiltsie, Judyann, Chung, Christine C, Gibson, Jack T, Lisnock, JeanMarie, Murphy, Beth A, Gorski, Judith N, Liu, Jinqi, Chen, Dunlu, Chen, Xiaoli, Wolff, Michael, Tong, Sharon X, Madeira, Maria, Karanam, Bindhu V, Shen, Dong-Ming, Balkovec, James M, Pinto, Shirly, Nargund, Ravi P, DeVita, Robert J

“…We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. In…”
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Discovery of imidazole carboxamides as potent and selective CCK1R agonists by Zhu, Cheng, Hansen, Alexa R., Bateman, Thomas, Chen, Zhesheng, Holt, Tom G., Hubert, James A., Karanam, Bindhu V., Lee, Susan J., Pan, Jie, Qian, Su, Reddy, Vijay B.G., Reitman, Marc L., Strack, Alison M., Tong, Vincent, Weingarth, Drew T., Wolff, Michael S., MacNeil, Doug J., Weber, Ann E., Duffy, Joseph L., Edmondson, Scott D.

“…The discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides as CCK1R agonists are reported. Compound 44 exhibited excellent lean mouse…”
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In vitro metabolism of MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl)-phe nyl] methyl]benzamide], a peroxisome proliferator-activated receptor α/γ agonist. II. Identification of metabolites by liquid chromatography-tandem mass spectrometry by LIU, David Q, KARANAM, Bindhu V, DOSS, George A, SIDLER, Rick R, VINCENT, Stella H, HOP, Cornelis E. C. A

“…The in vitro metabolism of MK-0767 [(+/-)-5-[(2,4-dioxothiazolidin-5-yl) methyl]-2-methoxy-N-[[(4-trifluoromethyl)-phenyl] methyl]benzamide], a novel…”
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In vitro metabolism of MK-0767 [(±)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl) phenyl]methyl]benzamide], a peroxisome proliferator-activated receptor α/γ agonist. I. Role of cytochrome P450, methyltransferases, flavin monooxygenases, and esterases by KARANAM, Bindhu V, HOP, Cornelis E. C. A, LIU, David Q, WALLACE, Mike, DEAN, Dennis, SATOH, Hiroya, KOMURO, Masakatsu, AWANO, Katsuya, VINCENT, Stella H

“…The metabolism of MK-0767, (+/-)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl) phenyl]methyl]benzamide, a thiazolidinedione…”
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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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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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In vitro metabolism of FK-506 in rat, rabbit, and human liver microsomes: identification of a major metabolite and of cytochrome P450 3A as the major enzymes responsible for its metabolism by Vincent, S H, Karanam, B V, Painter, S K, Chiu, S H

“…The metabolism of the immunosuppressant FK-506 was shown to be catalyzed primarily by cytochrome P450 isozymes of the P450 3A subfamily. Antibodies against rat…”
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Imidazopyridines: A novel class of hNav1.7 channel blockers by London, Clare, Hoyt, Scott B., Parsons, William H., Williams, Brande S., Warren, Vivien A., Tschirret-Guth, Richard, Smith, McHardy M., Priest, Birgit T., McGowan, Erin, Martin, William J., Lyons, Kathryn A., Li, Xiaohua, Karanam, Bindhu V., Jochnowitz, Nina, Garcia, Maria L., Felix, John P., Dean, Brian, Abbadie, Catherine, Kaczorowski, Gregory J., Duffy, Joseph L.

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