Search Results - "Dasgupta, Malini"

ADME optimization and toxicity assessment in early- and late-phase drug discovery by Caldwell, Gary W, Yan, Zhengyin, Tang, Weimin, Dasgupta, Malini, Hasting, Becki

“…Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in…”
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Isobaric metabolite interferences and the requirement for close examination of raw data in addition to stringent chromatographic separations in liquid chromatography/tandem mass spectrometric analysis of drugs in biological matrix by Yan, Zhengyin, Maher, Noureddine, Torres, Rhoda, Cotto, Carlos, Hastings, Becki, Dasgupta, Malini, Hyman, Rolanda, Huebert, Norman, Caldwell, Gary W.

“…In addition to matrix effects, common interferences observed in liquid chromatography/tandem mass spectrometry (LC/MS/MS) analyses can be caused by the…”
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Inside Cover Picture: Plasma Process. Polym. 5/2020 by Dasgupta, Malini, Fortugno, Paolo, Wiggers, Hartmut

“…Inside Front Cover: Silicon nanoparticles produced in a microwave‐assisted plasma reactor are subjected to in‐line functionalization in the plasma after‐glow…”
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Exploring the Si-precursor composition for inline coating and agglomeration of TiO2 via modular spray-flame and plasma reactor by López-Cámara, Claudia-Francisca, Dasgupta, Malini, Fortugno, Paolo, Wiggers, Hartmut

“…Inline particle coating after the particle formation process to preserve its specific properties is hardly investigated scientifically. Tackling that issue, we…”
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Plasma‐assisted gas‐phase synthesis and in‐line coating of silicon nanoparticles by Dasgupta, Malini, Fortugno, Paolo, Wiggers, Hartmut

“…This study investigates the feasibility of plasma‐supported in‐line functionalization of silicon nanoparticles (NPs) in an atmospheric pressure gas‐phase…”
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IGF-I supports the survival and/or differentiation of multiple types of central nervous system neurons by Bozyczko-Coyne, D, Glicksman, M A, Prantner, J E, McKenna, B, Connors, T, Friedman, C, Dasgupta, M, Neff, N T

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K-252a and staurosporine promote choline acetyltransferase activity in rat spinal cord cultures by Glicksman, M A, Prantner, J E, Meyer, S L, Forbes, M E, Dasgupta, M, Lewis, M E, Neff, N

“…The protein kinase inhibitor K-252a increased choline acetyltransferase (ChAT) activity in rat embryonic spinal cord cultures in a dose-dependent manner (EC50…”
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Use of stable isotope labeled probes to facilitate liquid chromatography/mass spectrometry based high-throughput screening of time-dependent CYP inhibitors by Dasgupta, Malini, Tang, Weimin, Caldwell, Gary W., Yan, Zhengyin

“…Inhibition curve shift is a commonly used approach for screening of time‐dependent CYP inhibitors which requires parallel paired incubations to obtain two…”
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Design, Synthesis, and Biological Evaluation of Novel Potent and Selective αvβ3/αvβ5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core by Marugán, Juan José, Manthey, Carl, Anaclerio, Beth, Lafrance, Lou, Lu, Tianbao, Markotan, Tom, Leonard, Kristi A, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce

“…A novel series of potent and selective αvβ3/αvβ5 dualinhibitors was designed, synthesized, and evaluated against several integrins. These compounds were…”
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Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif by Kreutter, Kevin D., Lu, Tianbao, Lee, Lily, Giardino, Edward C., Patel, Sharmila, Huang, Hui, Xu, Guozhang, Fitzgerald, Mark, Haertlein, Barbara J., Mohan, Venkatraman, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, McMillan, Martin, Spurlino, John C., Huebert, Norman D., Maryanoff, Bruce E., Tomczuk, Bruce E., Damiano, Bruce P., Player, Mark R.

“…2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated…”
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Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors by Qiao, Lei, Baumann, Christian A., Crysler, Carl S., Ninan, Nisha S., Abad, Marta C., Spurlino, John C., DesJarlais, Renee L., Kervinen, Jukka, Neeper, Mike P., Bayoumy, Shariff S., Williams, Robyn, Deckman, Ingrid C., Dasgupta, Malini, Reed, Rolanda L., Huebert, Norman D., Tomczuk, Bruce E., Moriarty, Kevin J.

“…The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of…”
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Pharmacokinetic properties of TDP4815 after single intravenous and oral administrations to rat, rabbit, monkey, dog and in vitro drug metabolism by Chen, Yanmin, Cheng, Deping, Tio, Cesar, Kagan, Natashia, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce, Bone, Roger, Huebert, Norman

“…The pharmacokinetics of TDP4815 was evaluated in rats, rabbits, dogs and monkeys. After intravenous administration, TDP4815 achieved CO of 3255 ng/ml in rats…”
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Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors by Tomczuk, Bruce, Lu, Tianbao, Soll, Richard M, Fedde, Cynthia, Wang, Aihua, Murphy, Larry, Crysler, Carl, Dasgupta, Malini, Eisennagel, Stephen, Spurlino, John, Bone, Roger

“…Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and…”
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Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core by Marugán, Juan José, Manthey, Carl, Anaclerio, Beth, Lafrance, Lou, Lu, Tianbao, Markotan, Tom, Leonard, Kristi A, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce

“…A novel series of potent and selective alpha(v)beta(3)/alpha(v)beta(5) dual( )()inhibitors was designed, synthesized, and evaluated against several integrins…”
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Design, Synthesis, and Biological Evaluation of Novel Potent and Selective α v β 3 /α v β 5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core by Marugán, Juan José, Manthey, Carl, Anaclerio, Beth, Lafrance, Lou, Lu, Tianbao, Markotan, Tom, Leonard, Kristi A., Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce

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Using in vitro human tissues to predict pharmacokinetic properties by Huebert, Norman D, Dasgupta, Malini, Chen, Yanmin

“…Pressure on drug discovery teams to predict the success of drug candidates earlier in the drug discovery process has led to the development of in vitro assays…”
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