Search Results - "Civiello, Rita"

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core by Sivaprakasam, Prasanna, Han, Xiaojun, Civiello, Rita L, Jacutin-Porte, Swanee, Kish, Kevin, Pokross, Matt, Lewis, Hal A, Ahmed, Nazia, Szapiel, Nicolas, Newitt, John A, Baldwin, Eric T, Xiao, Hong, Krause, Carol M, Park, Hyunsoo, Nophsker, Michelle, Lippy, Jonathan S, Burton, Catherine R, Langley, David R, Macor, John E, Dubowchik, Gene M

“…Glycogen synthase kinase-3 (GSK-3) has been proposed to play a crucial role in the pathogenesis of many diseases including cancer, stroke, bipolar disorders,…”
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Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines by Civiello, Rita L., Han, Xiaojun, Beno, Brett R., Chaturvedula, Prasad V., Herbst, John J., Xu, Cen, Conway, Charles M., Macor, John E., Dubowchik, Gene M.

“…[Display omitted] Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP…”
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Respiratory syncytial virus fusion inhibitors. Part 7: Structure–activity relationships associated with a series of isatin oximes that demonstrate antiviral activity in vivo by Sin, Ny, Venables, Brian L., Combrink, Keith D., Gulgeze, H. Belgin, Yu, Kuo-Long, Civiello, Rita L., Thuring, Jan, Wang, X. Alan, Yang, Zheng, Zadjura, Lisa, Marino, Anthony, Kadow, Kathleen F., Cianci, Christopher W., Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Krystal, Mark, Meanwell, Nicholas A.

“…A series of bezimidazole-isatin oximes were prepared and profiled as inhibitors of respiratory syncytial virus (RSV) replication in cell culture…”
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The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2 by Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Degnan, Andrew P., Jiang, Xiang-Jun, Macci, Robert, Mathias, Neil R., Moench, Paul, Pin, Sokhom S., Schartman, Richard, Signor, Laura J., Thalody, George, Tora, George, Whiterock, Valerie, Xu, Cen, Macor, John E., Dubowchik, Gene M.

“…Various substituted indazole and benzoxazolone amino acids were investigated as d-tyrosine surrogates in highly potent CGRP receptor antagonists. Compound 3,…”
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Catalytic Asymmetric Syntheses of α-Amino and α-Hydroxyl Acid Derivatives by Han, Xiaojun, Jiang, Xiang-Jun, Civiello, Rita L, Degnan, Andrew P, Chaturvedula, Prasad V, Macor, John E, Dubowchik, Gene M

“…Herein we report the first room temperature Heck reaction of aryl bromides and CH2C(NHP)CO2Me (P = Boc or CBz) to form ArCHC(NHP)CO2Me, which are then used…”
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Orally Active Fusion Inhibitor of Respiratory Syncytial Virus by Cianci, Christopher, Yu, Kuo-Long, Combrink, Keith, Sin, Ny, Pearce, Bradley, Wang, Alan, Civiello, Rita, Voss, Stacey, Luo, Guangxiang, Kadow, Kathy, Genovesi, Eugene V, Venables, Brian, Gulgeze, Hatice, Trehan, Ashok, James, Jennifer, Lamb, Lucinda, Medina, Ivette, Roach, Julia, Yang, Zheng, Zadjura, Lisa, Colonno, Richard, Clark, Junius, Meanwell, Nicholas, Krystal, Mark

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1 by Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Macci, Robert, Pin, Sokhom S., Ren, Shelly X., Schartman, Richard, Signor, Laura J., Thalody, George, Widmann, Kimberly A., Xu, Cen, Chaturvedula, Prasad V., Macor, John E., Dubowchik, Gene M.

“…We have systematically studied the effects of varying the central unnatural amino acid moiety on CGRP receptor antagonist potency and CYP inhibition in a…”
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Respiratory syncytial virus fusion inhibitors. Part 4: Optimization for oral bioavailability by Yu, Kuo-Long, Sin, Ny, Civiello, Rita L., Wang, X. Alan, Combrink, Keith D., Gulgeze, H. Belgin, Venables, Brian L., Wright, J.J. Kim, Dalterio, Richard A., Zadjura, Lisa, Marino, Anthony, Dando, Sandra, D’Arienzo, Celia, Kadow, Kathleen F., Cianci, Christopher W., Li, Zhufang, Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Colonno, Richard J., Yang, Zheng, Krystal, Mark, Meanwell, Nicholas A.

“…A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and…”
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Respiratory syncytial virus fusion inhibitors. Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity by Wang, Xiangdong Alan, Cianci, Christopher W., Yu, Kuo-Long, Combrink, Keith D., Thuring, Jan W., Zhang, Yi, Civiello, Rita L., Kadow, Kathleen F., Roach, Julia, Li, Zhufang, Langley, David R., Krystal, Mark, Meanwell, Nicholas A.

“…Extensive SAR studies and optimization of ADME properties of benzimidazol-2-one derivatives led to the identification of BMS-433771 (3) as an orally active RSV…”
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Catalytic Asymmetric Syntheses of Tyrosine Surrogates by Han, Xiaojun, Civiello, Rita L, Fang, Haiquang, Wu, Dedong, Gao, Qi, Chaturvedula, Prasad V, Macor, John E, Dubowchik, Gene M

“…Amino acid esters 5−11 as tyrosine mimics have been synthesized in excellent enantioselectivity (up to 99.6% ee) and in good overall chemical yields. The key…”
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Respiratory syncytial virus fusion inhibitors. Part 6: An examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety by Combrink, Keith D., Gulgeze, H. Belgin, Thuring, Jan W., Yu, Kuo-Long, Civiello, Rita L., Zhang, Yi, Pearce, Bradley C., Yin, Zhiwei, Langley, David R., Kadow, Kathleen F., Cianci, Christopher W., Li, Zhufang, Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Yang, Zheng, Zadjura, Lisa, Krystal, Mark, Meanwell, Nicholas A.

“…The effect of structural variation of the benzimidazol-2-one ring of RSV fusion inhibitors related to BMS-433771 ( 1) was examined in conjunction with side…”
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Fundamental structure–Activity relationships associated with a new structural class of respiratory syncytial virus inhibitor by Yu, Kuo-Long, Zhang, Yi, Civiello, Rita L., Kadow, Kathleen F., Cianci, Christopher, Krystal, Mark, Meanwell, Nicholas A.

“…Structure–activity relationships surrounding the dialkylamino side chain of a series of benzotriazole-derived inhibitors of respiratory syncytial virus fusion…”
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Syntheses of aza and fluorine-substituted 3-(piperidin-4-yl)-4,5-dihydro-1H-benzo[d][1,3]diazepin-2(3H)-ones by Han, Xiaojun, Civiello, Rita L., Mercer, Stephen E., Macor, John E., Dubowchik, Gene M.

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Respiratory syncytial virus fusion inhibitors. Part 3: Water-soluble benzimidazol-2-one derivatives with antiviral activity in vivo by Yu, Kuo-Long, Wang, Xiangdong Alan, Civiello, Rita L., Trehan, Ashok K., Pearce, Bradley C., Yin, Zhiwei, Combrink, Keith D., Gulgeze, H. Belgin, Zhang, Yi, Kadow, Kathleen F., Cianci, Christopher W., Clarke, Junius, Genovesi, Eugene V., Medina, Ivette, Lamb, Lucinda, Wyde, Philip R., Krystal, Mark, Meanwell, Nicholas A.

“…The introduction of acidic and basic functionality into the side chains R and R′ of respiratory syncytial virus (RSV) fusion inhibitors 2 was examined in an…”
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Respiratory syncytial virus inhibitors. Part 2: Benzimidazol-2-one derivatives by YU, Kuo-Long, YI ZHANG, CIANCI, Christopher W, KRYSTAL, Mark, MEANWELL, Nicholas A, CIVIELLO, Rita L, TREHAN, A. Ashok K, PEARCE, Bradley C, ZHIWEI YIN, COMBRINK, Keith D, GULGEZE, H. Belgin, WANG, Xiangdong Alan, KADOW, Kathleen F

“…Structure-activity relationships for a series of benzimidazol-2-one-based inhibitors of respiratory syncytial virus are described. These studies focused on…”
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Asymmetric Synthesis of Sesaminone:  Confirmation of Its Structure and Determination of Its Absolute Configuration by Maioli, Andrew T, Civiello, Rita L, Foxman, Bruce M, Gordon, Dana M

“…An asymmetric synthesis of the naturally occurring antipode of the tetrahydrofuran lignan sesaminone ((−)-1) has been achieved. An X-ray crystal structure of…”
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An efficient synthesis of N-arylated, orthogonally protected racemic aspartates by Luo, Guanglin, Chen, Ling, Civiello, Rita, Dubowchik, Gene M.

“…A brief and efficient synthesis of various N-arylated racemic aspartates has been achieved by two consecutive reactions in one-pot, in which imine or…”
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Calcitonin gene-related peptide (CGRP) receptor antagonists: Pyridine as a replacement for a core amide group by Luo, Guanglin, Chen, Ling, Civiello, Rita, Pin, Sokhom S., Xu, Cen, Kostich, Walter, Kelley, Michelle, Conway, Charles M., Macor, John E., Dubowchik, Gene M.

“…In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a…”
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Corrigendum to “The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2” [Bioorg. Med. Chem. Lett. 23 (2013) 1870–1873] by Han, Xiaojun, Civiello, Rita L., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Degnan, Andrew P., Jiang, Xiang-Jun, Macci, Robert, Mathias, Neil R., Moench, Paul, Pin, Sokhom S., Schartman, Richard, Signor, Laura J., Thalody, George, Tora, George, Whiterock, Valerie, Xu, Cen, Macor, John E., Dubowchik, Gene M.

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Syntheses of aza and fluorine-substituted 3-(piperidin-4-yl)-4,5-dihydro-1 H-benzo[ d][1,3]diazepin-2(3 H)-ones by Han, Xiaojun, Civiello, Rita L., Mercer, Stephen E., Macor, John E., Dubowchik, Gene M.

“…The title compounds 2 and 3 were formed in good to excellent overall yields by Michael addition of a primary amine to activated vinyl groups in 5 and 11, by…”
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