Search Results - "Taunk, Prakash"

Discovery and Preclinical Profile of Saxagliptin (BMS-477118):  A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes by Augeri, David J, Robl, Jeffrey A, Betebenner, David A, Magnin, David R, Khanna, Ashish, Robertson, James G, Wang, Aiying, Simpkins, Ligaya M, Taunk, Prakash, Huang, Qi, Han, Song-Ping, Abboa-Offei, Benoni, Cap, Michael, Xin, Li, Tao, Li, Tozzo, Effie, Welzel, Gustav E, Egan, Donald M, Marcinkeviciene, Jovita, Chang, Shu Y, Biller, Scott A, Kirby, Mark S, Parker, Rex A, Hamann, Lawrence G

“…Efforts to further elucidate structure−activity relationships (SAR) within our previously disclosed series of β-quaternary amino acid linked…”
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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP) by Sulsky, Richard, Magnin, David R., Huang, Yanting, Simpkins, Ligaya, Taunk, Prakash, Patel, Manorama, Zhu, Yeheng, Stouch, Terry R., Bassolino-Klimas, Donna, Parker, Rex, Harrity, Thomas, Stoffel, Robert, Taylor, David S., Lavoie, Thomas B., Kish, Kevin, Jacobson, Bruce L., Sheriff, Steven, Adam, Leonard P., Ewing, William R., Robl, Jeffrey A.

“…X-ray crystal structure of an FABP inhibitor bound to the active site of aFABP. Herein we report the first disclosure of biphenyl azoles that are nanomolar…”
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Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability:  Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-l-cis-4,5-methanoprolinenitrile-Based Inhibitors by Magnin, David R, Robl, Jeffrey A, Sulsky, Richard B, Augeri, David J, Huang, Yanting, Simpkins, Ligaya M, Taunk, Prakash C, Betebenner, David A, Robertson, James G, Abboa-Offei, Benoni E, Wang, Aiying, Cap, Michael, Xin, Li, Tao, Li, Sitkoff, Doree F, Malley, Mary F, Gougoutas, Jack Z, Khanna, Ashish, Huang, Qi, Han, Song-Ping, Parker, Rex A, Hamann, Lawrence G

“…A series of methanoprolinenitrile-containing dipeptide mimetics were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease…”
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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors by Zhao, Guohua, Taunk, Prakash C., Magnin, David R., Simpkins, Ligaya M., Robl, Jeffrey A., Wang, Aiying, Robertson, James G., Marcinkeviciene, Jovita, Sitkoff, Doree F., Parker, Rex A., Kirby, Mark S., Hamann, Lawrence G.

“…Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma…”
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Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1 by Magnin, David R., Taunk, Prakash C., Robertson, James G., Wang, Aiying, Marcinkeviciene, Jovita, Kirby, Mark S., Hamann, Lawrence G.

“…The synthesis and dipeptidyl peptidase IV inhibitory activity of glycine- and alaninenitrile dipeptides are reported. A series of…”
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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors by Robl, Jeffrey A, Sulsky, Richard, Sun, Chong-Qing, Simpkins, Ligaya M, Wang, Tammy, Dickson, John K, Chen, Ying, Magnin, David R, Taunk, Prakash, Slusarchyk, William A, Biller, Scott A, Lan, Shih-Jung, Connolly, Fergal, Kunselman, Lori K, Sabrah, Talal, Jamil, Haris, Gordon, David, Harrity, Thomas W, Wetterau, John R

“…A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in…”
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Application of robotics to steady state enzyme kinetics: analysis of tight-binding inhibitors of dipeptidyl peptidase IV by Wang, Aiying, Huang, Yanting, Taunk, Prakash, Magnin, David R, Ghosh, Krishnendu, Robertson, James G

“…Using available commercial robotics and instrumentation, we developed a fully automated and rigorous steady state enzyme kinetic assay for dipeptidyl peptidase…”
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Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents by Magnin, David R, Biller, Scott A, Wetterau, John, Robl, Jeffrey A, Dickson, John K, Taunk, Prakash, Harrity, Thomas W, Lawrence, R.Michael, Sun, C.-Q, Wang, Tammy, Logan, Janette, Fryszman, Olga, Connolly, Fergal, Jolibois, Kern, Kunselman, Lori

“…A series of newly synthesized phosphonate esters were evaluated for their effects on microsomal triglyceride transfer protein activity (MTP). The most potent…”
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Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR by Barrish, J C, Gordon, E, Alam, M, Lin, P F, Bisacchi, G S, Chen, P, Cheng, P T, Fritz, A W, Greytok, J A, Hermsmeier, M A

“…A series of HIV protease inhibitors containing a novel C2 symmetrical "aminodiol" core structure were prepared from amino acid starting materials. The ability…”
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Dual metalloprotease inhibitors.v. Utilization of bicyclic azepinonethiazolidines and azepinonetetrahydrothiazines in constrained peptidomimetics of mercaptoacyl dipeptides by Slusarchyk, William A., Robl, Jeffrey A., Taunk, Prakash C., Assad, Magdi M., Bird, J.Eileen, DiMarco, John, Pan, Yolanda

“…Incorporation of mercaptoacetyl or mercaptopropanoyl groups into azepinonethiazolidine and azepinonetetrahydrothiazine carboxylic acids provided…”
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New tetracyclic ring systems. Synthesis of 1 H ‐oxazolo[5,4,3‐ kl ]phenothiazines and [1,4]oxazino[2,3,4‐ kl ]phenothiazines by Nodiff, Edward A., Taunk, Prakash C.

“…Abstract 1‐Hydroxyphenothiazine was converted to 1 H ‐oxazolo[5,4,3‐ kl ]phenothiazin‐1‐one, 1 H ‐oxazolo[5,4,3‐ kl…”
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Synthesis of a new benzo[a]phenothiazine amino alcohol as a proposed antimalarial by Taunk, Prakash C.

“…The synthesis of α‐(di‐n‐butylaminomethyl)‐2‐benzo[a]phenothiazinyl methanol hydrochloride is described. The ir and nmr spectra are also included…”
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New tetracyclic ring systems. Synthesis of 1H-oxazolo[5,4,3-kl]phenothiazines and [1,4]oxazino[2,3,4-kl]phenothiazines by Nodiff, Edward A., Taunk, Prakash C.

“…1‐Hydroxyphenothiazine was converted to 1H‐oxazolo[5,4,3‐kl]phenothiazin‐1‐one,…”
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Die Synthese von 2-Amino-5-fluorthiophenol und seine Umwandlung in Phenothiazine und deren Sulfone by Mital, R. L., Taunk, Prakash Chand

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