共查询到20条相似文献，搜索用时 15 毫秒
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James Adams Edward&#;C. Anderson Emma E. Blackham Yin Wa Ryan Chiu Thomas Clarke Natasha Eccles Luke A. Gill Joshua J. Haye Harvey T. Haywood Christian R. Hoenig Marius Kausas Joelle Le Hannah L. Russell Christopher Smedley William J. Tipping Tom Tongue Charlotte C. Wood Jason Yeung James E. Rowedder M. Jonathan Fray Thomas McInally Simon J. F. Macdonald 《ACS medicinal chemistry letters》2014,5(11):1207-1212
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Francesca Brunelli Chiara Ceresa Letizia Fracchia Gian Cesare Tron Silvio Aprile 《ACS medicinal chemistry letters》2022,13(12):1898
With their three points of diversity, α-acyloxy carboxamides, which are accessible with the Passerini reaction, provide heterogeneity for the preparation of libraries of putative active agents or intermediates used for the formation of more complex structures. If on the one hand the presence of a hydrolyzable ester function has been exploited to design both prodrugs and soft drugs, on the other hand medicinal chemists are reluctant to use this skeleton to prepare hard drugs. Herein we investigated whether the stability of the ester could be controlled, leading to the formation of hydrolytically stable α-acyloxy carboxamides. When the group directly attached to the ester moiety (R3) is an ortho-substituted or ortho,ortho′-disubstituted aromatic ring, α-acyloxy carboxamides are stable. In human liver but not in rodents, due to the different expression of esterases, the ester function is also stable toward hydrolysis when the R1 group is a bulky substituent regardless of the nature of the R3 substituent. 相似文献
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Hongbing Huang Lisa Acquaviva Virginia Berry Howard Bregman Nagasree Chakka Anne O’Connor Erin F. DiMauro Jennifer Dovey Oleg Epstein Barbara Grubinska Jon Goldstein Hakan Gunaydin Zihao Hua Xin Huang Liyue Huang Jason Human Alex Long John Newcomb Vinod&#;F. Patel Doug Saffran Randy Serafino Steve Schneider Craig Strathdee Jin Tang Susan Turci Ryan White Violeta Yu Huilin Zhao Cindy Wilson Matthew&#;W. Martin 《ACS medicinal chemistry letters》2012,3(12):1059-1064
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Matic Proj Martina Hrast Damijan Knez Kri&#x;tof Bozovi
ar Katarina Grabrijan Ane Meden Stanislav Gobec Rok Frlan 《ACS medicinal chemistry letters》2022,13(12):1905
Thiazoles exhibit a wide range of biological activities and therefore represent useful and attractive building blocks. To evaluate their usefulness and pinpoint their liabilities in fragment screening campaigns, we assembled a focused library of 49 fragment-sized thiazoles and thiadiazoles with various substituents, namely amines, bromides, carboxylic acids, and nitriles. The library was profiled in a cascade of biochemical inhibition assays, redox activity, thiol reactivity, and stability assays. Our study indicates that when thiazole derivatives are identified as screening hits, their reactivity should be carefully addressed and correlated with specific on-target engagement. Importantly, nonspecific inhibition should be excluded using experimental approaches and in silico predictions. To help with validation of hits identified in fragment screening campaigns, we can apply our high-throughput profiling workflow to focus on the most tractable compounds with a clear mechanism of action. 相似文献
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Wen-Lian Wu Martin Domalski Duane&#;A. Burnett Hubert Josien Thomas Bara Murali Rajagopalan Ruo Xu John Clader William J. Greenlee Andrew Brunskill Lynn&#;A. Hyde Robert A. Del Vecchio Mary E. Cohen-Williams Lixin Song Julie Lee Giuseppe Terracina Qi Zhang Amin Nomeir Eric&#;M. Parker Lili Zhang 《ACS medicinal chemistry letters》2012,3(11):892-896
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Mariangela Ceruso Sonia Del Prete Zeid Alothman Clemente Capasso Claudiu T. Supuran 《ACS medicinal chemistry letters》2014,5(7):826-830
l-lysine or GABA
scaffolds and the conversion of the terminal amino group to the guanidine
one, benzenesulfonamides incorporating water solubilizing moieties
were synthesized. The new compounds were medium potency inhibitors
of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and
II, and highly effective, nanomolar inhibitors of the pathogenic bacterial
α-CA from Vibrio cholerae. These sulfonamides
possess good selectivity for inhibiting the bacterial over the mammalian
isoforms and may be used as tools to understand the role of bacterial
CAs in pathogenesis. 相似文献