- Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against: Klebsiella pneumoniae
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A series of fused bicyclic 2-aminothiazolyl compounds were synthesized and evaluated for their synergistic effects with polymyxin B (PB) against Klebsiella pneumoniae (SIPI-KPN-1712). Some of the synthesized compounds exhibited synergistic activity. When 4 μg ml-1 compound B1 was combined with PB, it showed potent antibacterial activity, achieving 64-fold reduction of the MIC of PB. Furthermore, compound B1 showed prominent synergistic efficacy in both concentration gradient and time-kill curves in vitro. In addition, B1 combined with PB also exhibited synergistic and partial synergistic effect against E. coli (ATCC25922 and its clinical isolates), Acinetobacter baumannii (ATCC19606 and its clinical isolates), and Pseudomonas aeruginosa (Pae-1399).
- Wang, Rong,Hou, Shuang,Dong, Xiaojing,Chen, Daijie,Shao, Lei,Qian, Liujia,Li, Zhong,Xu, Xiaoyong
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supporting information
p. 2060 - 2066
(2017/11/22)
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- Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
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A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 3 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma.
- Das, Jagabandhu,Furch, Joseph A.,Liu, Chunjian,Moquin, Robert V.,Lin, James,Spergel, Steven H.,McIntyre, Kim W.,Shuster, David J.,O'Day, Kathleen D.,Penhallow, Becky,Hung, Chen-Yi,Doweyko, Arthur M.,Kamath, Amrita,Zhang, Hongjian,Marathe, Punit,Kanner, Steven B.,Lin, Tai-An,Dodd, John H.,Barrish, Joel C.,Wityak, John
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p. 3706 - 3712
(2007/10/03)
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- Polycyclic thiazoles as potassium ion channel modulators
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The present invention provides a genus of polycyclic thiazoles that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
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Page/Page column 15
(2008/06/13)
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- GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS
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The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.
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Page/Page column 73
(2010/02/13)
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