Search Results - "Gu, Yu Gui"

Influenza Neuraminidase Inhibitors:  Structure-Based Design of a Novel Inhibitor Series by Stoll, Vincent, Stewart, Kent D, Maring, Clarence J, Muchmore, Steven, Giranda, Vincent, Gu, Yu-gui Y, Wang, Gary, Chen, Yuanwei, Sun, Minghua, Zhao, Chen, Kennedy, April L, Madigan, Darold L, Xu, Yibo, Saldivar, Ayda, Kati, Warren, Laver, Graeme, Sowin, Thomas, Sham, Hing L, Greer, Jonathan, Kempf, Dale

“…Combinatorial and structure-based medicinal chemistry strategies were used together to advance a lead compound with an activity of K i = 58 μM via a potency…”
Get full text

Structure-based Optimization of MurF Inhibitors by Stamper, Geoffrey F., Longenecker, Kenton L., Fry, Elizabeth H., Jakob, Clarissa G., Florjancic, Alan S., Gu, Yu-Gui, Anderson, David D., Cooper, Curt S., Zhang, Tianyuan, Clark, Richard F., Cia, Yingna, Black-Schaefer, Candace L., Owen McCall, J., Lerner, Claude G., Hajduk, Philip J., Beutel, Bruce A., Stoll, Vincent S.

“…The d‐Ala‐d‐Ala adding enzyme (MurF) from Streptococcus pneumoniae catalyzes the ATP‐dependent formation of the UDP‐MurNAc‐pentapeptide, a critical component…”
Get full text

Design, synthesis and structure–activity relationships of 6-O-arylpropargyl diazalides with potent activity against multidrug-resistant Streptococcus pneumoniae by Yong, Hong, Gui Gu, Yu, Clark, Richard F., Marron, Thomas, Ma, Zhenkun, Soni, Niru, Stone, Gregory G., Nilius, Angela M., Marsh, Kennan, Djuric, Stevan W.

“…A novel series of 6-O-arylpropargyl diazalides was synthesized and evaluated for their antibacterial activity. Members of this series exhibited potent activity…”
Get full text

From Bacterial Genomes to Novel Antibacterial Agents: Discovery, Characterization, and Antibacterial Activity of Compounds that Bind to HI0065 (YjeE) from Haemophilus influenzae by Lerner, Claude G., Hajduk, Philip J., Wagner, Rolf, Wagenaar, Frank L., Woodall, Charlotte, Gu, Yu‐Gui, Searle, Xenia B., Florjancic, Alan S., Zhang, Tianyuan, Clark, Richard F., Cooper, Curt S., Mack, Jamey C., Yu, Liping, Cai, Mengli, Betz, Steven F., Chovan, Linda E., McCall, J. Owen, Black‐Schaefer, Candace L., Kakavas, Stephan J., Schurdak, Mark E., Comess, Kenneth M., Walter, Karl A., Edalji, Rohinton, Dorwin, Sarah A., Smith, Richard A., Hebert, Eric J., Harlan, John E., Metzger, Randy E., Merta, Philip J., Baranowski, John L., Coen, Michael L., Thornewell, Susan J., Shivakumar, Annapur G., Saiki, Anne Y., Soni, Niru, Bui, Mai, Balli, Darlene J., Sanders, William J., Nilius, Angela M., Holzman, Thomas F., Fesik, Stephen W., Beutel, Bruce A.

“…As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR‐ and mass spectrometry‐based affinity selection screens…”
Get full text

An efficient chemical synthesis of carboxylate-isostere analogs of daptomycin by Yoganathan, Sabesan, Yin, Ning, He, Yong, Mesleh, Michael F, Gu, Yu Gui, Miller, Scott J

“…Herein we report a direct and efficient method for the synthesis of four new carboxylate-isostere analogs of daptomycin. The side chain carboxylic acid…”
Get more information

Gene expression analysis in rats treated with experimental acetyl-coenzyme A carboxylase inhibitors suggests interactions with the peroxisome proliferator-activated receptor alpha pathway by Waring, Jeffrey F, Yang, Yi, Healan-Greenberg, Christine H, Adler, Andrew L, Dickinson, Robert, McNally, Teresa, Wang, Xiaojun, Weitzberg, Moshe, Xu, Xiangdong, Lisowski, Andrew, Warder, Scott E, Gu, Yu Gui, Zinker, Bradley A, Blomme, Eric A, Camp, Heidi S

“…Acetyl CoA carboxylase (ACC) 2, which catalyzes the carboxylation of acetyl-CoA to form malonyl-CoA, has been identified as a potential target for type 2…”
Get more information

Studies of mild dehydrogenations in heterocyclic systems by Williams, David R., Lowder, Patrick D., Gu, Yu-Gui, Brooks, Dawn A.

“…The use of bromotrichloromethane-DBU is described for the selective oxidative conversion of several dihydro-heterocyclic systems to the corresponding…”
Get full text

Structure of MurF from Streptococcus pneumoniae co‐crystallized with a small molecule inhibitor exhibits interdomain closure by Longenecker, Kenton L., Stamper, Geoffrey F., Hajduk, Philip J., Fry, Elizabeth H., Jakob, Clarissa G., Harlan, John E., Edalji, Rohinton, Bartley, Diane M., Walter, Karl A., Solomon, Larry R., Holzman, Thomas F., Gu, Yu Gui, Lerner, Claude G., Beutel, Bruce A., Stoll, Vincent S.

“…In a broad genomics analysis to find novel protein targets for antibiotic discovery, MurF was identified as an essential gene product for Streptococcus…”
Get full text

Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents by Clark, Richard F., Zhang, Tianyuan, Wang, Xiaojun, Wang, Rongqi, Zhang, Xiaolin, Camp, Heidi S., Beutel, Bruce A., Sham, Hing L., Gu, Yu Gui

“…Optimization studies aimed at improving the potency and selectivity profiles of a recently discovered series of acetyl-CoA carboxylase (ACC) inhibitors are…”
Get full text

Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3- d]pyrimidines as adenosine kinase inhibitors by Perner, Richard J., Lee, Chih-Hung, Jiang, Meiqun, Gu, Yu-Gui, DiDomenico, Stanley, Bayburt, Erol K., Alexander, Karen M., Kohlhaas, Kathy L., Jarvis, Michael F., Kowaluk, Elizabeth L., Bhagwat, Shripad S.

“…[Display omitted] The synthesis and structure–activity relationship of a series of 6,7-disubstituted 4-aminopyrido[2,3- d]pyrimidines as novel non-nucleoside…”
Get full text

trans-2,6-, 3,6- and 4,6-Diaza-5,6,6a,7,8,12b-hexahydrobenzo[ C]phenanthrene-10,11-diols as dopamine agonists by Gu, Yu Gui, Bayburt, Erol K., Michaelides, Michael R., Lin, Chun Wei, Shiosaki, Kazumi

“…The title compounds were synthesized by replacing the thiophene moiety of A-86929( 2a) with variously substituted pyridines. Dopamine D-1 and D-2 binding and…”
Get full text

Synthesis and Structure−Activity Relationships of N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy Derivatives as Selective Acetyl-CoA Carboxylase 2 Inhibitors by Gu, Yu Gui, Weitzberg, Moshe, Clark, Richard F, Xu, Xiangdong, Li, Qun, Zhang, Tianyuan, Hansen, T. Matthew, Liu, Gang, Xin, Zhili, Wang, Xiaojun, Wang, Rongqi, McNally, Teresa, Camp, Heidi, Beutel, Bruce A, Sham, Hing L

“…A structurally novel acetyl-CoA carboxylase (ACC) inhibitor is identified from high-throughput screening. A preliminary structure−activity relationship study…”
Get full text

Studies toward funiculosin. Intramolecular carbonyl condensations using carboxamidimidazolide intermediates by Williams, David R., Lowder, Patrick D., Gu, Yu-Gui

“…Internal enolate condensations, utilizing carboxamidimidazoles as activated ureas, provide a general synthesis of the 3,5-disubstituted-4-hydroxy-2-pyridinone…”
Get full text

Structure-Based Characterization and Optimization of Novel Hydrophobic Binding Interactions in a Series of Pyrrolidine Influenza Neuraminidase Inhibitors by Maring, Clarence J, Stoll, Vincent S, Zhao, Chen, Sun, Minghua, Krueger, Allan C, Stewart, Kent D, Madigan, Darold L, Kati, Warren M, Xu, Yibo, Carrick, Robert J, Montgomery, Debra A, Kempf-Grote, Anita, Marsh, Kennan C, Molla, Akhteruzzaman, Steffy, Kevin R, Sham, Hing L, Laver, W. Graeme, Gu, Yu-gui, Kempf, Dale J, Kohlbrenner, William E

“…The structure−activity relationship (SAR) of a novel hydrophobic binding interaction within a subsite of the influenza neuraminidase (NA) active site was…”
Get full text

Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives by Matthew Hansen, T., Gu, Yu-Gui, Rehm, Tamara M., Dandliker, Peter J., Chovan, Linda E., Bui, Mai H., Nilius, Angela M., Beutel, Bruce A.

“…A series of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives were prepared and evaluated for cell-free bacterial protein…”
Get full text

N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy Derivatives as Acetyl-CoA Carboxylase InhibitorsImprovement of Cardiovascular and Neurological Liabilities via Structural Modifications by Gu, Yu Gui, Weitzberg, Moshe, Clark, Richard F, Xu, Xiangdong, Li, Qun, Lubbers, Nathan L, Yang, Yi, Beno, David W. A, Widomski, Deborah L, Zhang, Tianyuan, Hansen, T. Matthew, Keyes, Robert F, Waring, Jeffrey F, Carroll, Sherry L, Wang, Xiaojun, Wang, Rongqi, Healan-Greenberg, Christine H, Blomme, Eric A, Beutel, Bruce A, Sham, Hing L, Camp, Heidi S

“…A preliminary safety evaluation of ACC2 inhibitor 1-(S) revealed serious neurological and cardiovascular liabilities of this chemotype. A systematic…”
Get full text

Novel inhibitors of bacterial protein synthesis: structure–activity relationships for 1,8-naphthyridine derivatives incorporating position 3 and 4 variants by Clark, Richard F., Wang, Sanyi, Ma, Zhenkun, Weitzberg, Moshe, Motter, Christopher, Tufano, Michael, Wagner, Rolf, Gu, Yu-Gui, Dandliker, Peter J., Lerner, Claude G., Chovan, Linda E., Cai, Yingna, Black-Schaefer, Candace L., Lynch, Linda, Kalvin, Douglas, Nilius, Angela M., Pratt, Steve D., Soni, Niru, Zhang, Tianyuan, Zhang, Xiaolin, Beutel, Bruce A.

“…Graphic Structure–activity relationships for a recently discovered novel ribosome inhibitor (NRI) class of antibacterials were investigated. Preliminary…”
Get full text

Synthesis of 4-alkyl-3,5-dibromo-, 3-bromo-4,5-dialkyl- and 3,4,5-trialkylpyridines via sequential metalation and metal-halogen exchange of 3,5-dibromopyridine by Gu, Yu Gui, Bayburt, Erol K.

“…Lithiation of 3,5-dibromopyridine with LDA and subsequent reaction with electrophiles provided 4-alkyl-3,5-dibromopyridines 2 in high yield…”
Get full text

The synthesis and structure–activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications by Xu, Xiangdong, Weitzberg, Moshe, Keyes, Robert F., Li, Qun, Wang, Rongqi, Wang, Xiaojun, Zhang, Xiaolin, Frevert, Ernst U., Camp, Heidi S., Beutel, Bruce A., Sham, Hing L., Gu, Yu Gui

“…Potent and selective ACC2 inhibitors were synthesized by modifying the polar region of a HTS hit and the SAR suggests a compact and lipophilic binding pocket…”
Get full text

Discovery of 4-Amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine, an Orally Active, Non-Nucleoside Adenosine Kinase Inhibitor by Lee, Chih-Hung, Jiang, Meiqun, Cowart, Marlon, Gfesser, Greg, Perner, Richard, Kim, Ki Hwan, Gu, Yu Gui, Williams, Michael, Jarvis, Michael F, Kowaluk, Elizabeth A, Stewart, Andrew O, Bhagwat, Shripad S

“…Adenosine (ADO) is an endogenous homeostatic inhibitory neuromodulator that reduces cellular excitability at sites of tissue injury and inflammation…”
Get full text