Search Results - "BAKSHI, Raman K"

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist by Hong, Qingmei, Bakshi, Raman K., Palucki, Brenda L., Park, Min K., Ye, Zhixiong, He, Shuwen, Pollard, Patrick G., Sebhat, Iyassu K., Liu, Jian, Guo, Liangqin, Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.

“…We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound…”
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Highly enantioselective borane reduction of ketones catalyzed by chiral oxazaborolidines. Mechanism and synthetic implications by Corey, E. J, Bakshi, Raman K, Shibata, Saizo

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Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands by Bakshi, Raman K., Hong, Qingmei, Tang, Rui, Kalyani, Rubana N., MacNeil, Tanya, Weinberg, David H., Van der Ploeg, Lex H.T., Patchett, Arthur A., Nargund, Ravi P.

“…The design and synthesis of potent MC4 agonists 19b and 27 are reported. Design and synthesis of potent MC4 selective agonists based on cyclohexylpiperidine…”
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A stable and easily prepared catalyst for the enantioselective reduction of ketones. Applications to multistep syntheses by Corey, E. J, Bakshi, Raman K, Shibata, Saizo, Chen, Chung Pin, Singh, Vinod K

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An efficient and catalytically enantioselective route to (S)-(-)-phenyloxirane by Corey, E. J, Shibata, Saizo, Bakshi, Raman K

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1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: Application in the synthesis of potent human melanocortin-4 receptor selective agonists by Bakshi, Raman K., Hong, Qingmei, Olson, J.T., Ye, Zhixiong, Sebhat, Iyassue K., Weinberg, David H., MacNeil, Tanya, Kalyani, Rubana N., Tang, Rui, Martin, William J., Strack, Alison, McGowan, Erin, Tamvakopoulos, Constantin, Miller, Randy R., Stearns, Ralph A., Tang, Wei, Maclntyre, D. Euan, van der Ploeg, Lex H.T., Patchett, Arthur A., Nargund, Ravi P.

“…The discovery of 1-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid analogs as potent human melanocortin-4 selective agonists is described. The discovery…”
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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists by He, Shuwen, Dobbelaar, Peter H., Guo, Liangqin, Ye, Zhixiong, Liu, Jian, Jian, Tianying, Truong, Quang, Shah, Shrenik K., Du, Wu, Qi, Hongbo, Bakshi, Raman K., Hong, Qingmei, Dellureficio, James D., Sherer, Edward, Pasternak, Alexander, Feng, Zhe, Reibarkh, Mikhail, Lin, Melissa, Samuel, Koppara, Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J., Li, Cai, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Nargund, Ravi P., Hagmann, William K.

“…MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs. Additional investigations…”
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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain by Chobanian, Harry R, Guo, Yan, Liu, Ping, Chioda, Marc D, Fung, Selena, Lanza, Thomas J, Chang, Linda, Bakshi, Raman K, Dellureficio, James P, Hong, Qingmei, McLaughlin, Mark, Belyk, Kevin M, Krska, Shane W, Makarewicz, Amanda K, Martel, Elliot J, Leone, Joseph F, Frey, Lisa, Karanam, Bindhu, Madeira, Maria, Alvaro, Raul, Shuman, Joyce, Salituro, Gino, Terebetski, Jenna L, Jochnowitz, Nina, Mistry, Shruti, McGowan, Erin, Hajdu, Richard, Rosenbach, Mark, Abbadie, Catherine, Alexander, Jessica P, Shiao, Lin-Lin, Sullivan, Kathleen M, Nargund, Ravi P, Wyvratt, Matthew J, Lin, Linus S, DeVita, Robert J

“…We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening…”
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Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity by He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Bakshi, Raman K., Hong, Qingmei, Dellureficio, James P., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Reibarkh, Mikhail, Holmes, Mark A., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.

“…We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses…”
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Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists by He, Shuwen, Lai, Zhong, Ye, Zhixiong, Dobbelaar, Peter H, Shah, Shrenik K, Truong, Quang, Du, Wu, Guo, Liangqin, Liu, Jian, Jian, Tianying, Qi, Hongbo, Bakshi, Raman K, Hong, Qingmei, Dellureficio, James, Reibarkh, Mikhail, Samuel, Koppara, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J, Li, Cai, Zhang, Bei, Howard, Andrew D, Zhou, Yun-Ping, Nargund, Ravi P, Hagmann, William K

“…Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first…”
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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist by He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Tsou, Nancy N., Ball, Richard G., Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.

“…We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4…”
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Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity by He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Weinberg, David H., MacNeil, Tanya, Tang, Rui, Strack, Alison M., Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.

“…We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the…”
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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes by He, Shuwen, Ye, Zhixiong, Truong, Quang, Shah, Shrenik, Du, Wu, Guo, Liangqin, Dobbelaar, Peter H, Lai, Zhong, Liu, Jian, Jian, Tianying, Qi, Hongbo, Bakshi, Raman K, Hong, Qingmei, Dellureficio, James, Pasternak, Alexander, Feng, Zhe, deJesus, Reynalda, Yang, Lihu, Reibarkh, Mikhail, Bradley, Scott A, Holmes, Mark A, Ball, Richard G, Ruck, Rebecca T, Huffman, Mark A, Wong, Frederick, Samuel, Koppara, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Eiermann, George J, Li, Cai, Zhang, Bei B, Howard, Andrew D, Zhou, Yun-Ping, Nargund, Ravi P, Hagmann, William K

“…A structure–activity relationship study of the imidazolyl-β-tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which…”
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Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists by LIANGQIN GUO, ZHIXIONG YE, TSOU, Nancy N, BALL, Richard G, WEINBERG, David H, MACNEIL, Tanya, RUI TANG, TAMVAKOPOULOS, Constantin, QIANPING PENG, CHEN, Howard Y, CHEN, Airu S, MARTIN, William J, JIAN LIU, EUAN MACINTYRE, D, STRACK, Alison M, FONG, Tung M, WYVRATT, Matthew J, NARGUND, Ravi P, SHUWEN HE, BAKSHI, Raman K, SEBHAT, Iyassu K, DOBBELAAR, Peter H, QINGMEI HONG, TIANYING JIAN, DELLUREFICIO, James P

“…Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin…”
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Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands by Hong, Qingmei, Bakshi, Raman K., Dellureficio, James, He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Tang, Rui, Kalyani, Rubana N., MacNeil, Tanya, Vongs, Aurawan, Rosenblum, Charles I., Weinberg, David H., Peng, Qingping, Tamvakopoulos, Constantin, Miller, Randy R., Stearns, Ralph A., Cashen, Doreen, Martin, Willian J., Chen, Airu S., Metzger, Joseph M., Chen, Howard Y., Strack, Allison M., Fong, Tung M., Maclntyre, Euan, Van der Ploeg, Lex H.T., Wyvratt, Matthew J., Nargund, Ravi P.

“…Design, syntheses and structure–activity relationships of piperazine privileged structures containing MC4R agonist compounds 6 were described. The most potent…”
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Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride:  Enzyme-Catalyzed Formation of NADP−Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor by Bull, Herbert G, Garcia-Calvo, Margarita, Andersson, Stefan, Baginsky, Walter F, Chan, H. Karen, Ellsworth, Dina E, Miller, Randall R, Stearns, Ralph A, Bakshi, Raman K, Rasmusson, Gary H, Tolman, Richard L, Myers, Robert W, Kozarich, John W, Harris, Georgianna S

“…Finasteride is employed in treatment of benign prostatic hyperplasia in man, where its target enzyme is steroid 5α-reductase. It is a novel, potent…”
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Chiral synthesis via organoboranes. 10. Preparation of .alpha.-chiral acyclic ketones of exceptionally high enantiomeric excess from optically pure borinic esters by Brown, Herbert C, Srebnik, Morris, Bakshi, Raman K, Cole, Thomas E

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4-Aza-3-oxo-5.alpha.-androst-1-ene-17.beta.-N-arylcarboxamides as Dual Inhibitors of Human Type 1 and Type 2 Steroid 5.alpha.-Reductases. Dramatic Effect of N-Aryl Substituents on Type 1 and Type 2 5.alpha.-Reductase Inhibitory Potency by Bakshi, Raman K, Rasmusson, Gary H, Patel, Gool F, Mosley, Ralph T, Chang, Benedict, Ellsworth, Kenneth, Harris, Georgianna S, Tolman, Richard L

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Major effect of the leaving group in dialkylboron chlorides and triflates in controlling the stereospecific conversion of ketones into either [E]- or [Z]-enol borinates by Brown, Herbert C, Dhar, Raj K, Bakshi, Raman K, Pandiarajan, Paul K, Singaram, Bakthan

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Total synthesis of (.+-.)-atractyligenin by Singh, Ashok K, Bakshi, Raman K, Corey, E. J

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