101080-15-3Relevant academic research and scientific papers
Discovery of imidazo[2,1- b ]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents
Wang, Ning-Yu,Xu, Ying,Zuo, Wei-Qiong,Xiao, Kun-Jie,Liu, Li,Zeng, Xiu-Xiu,You, Xin-Yu,Zhang, Li-Dan,Gao, Chao,Liu, Zhi-Hao,Ye, Ting-Hong,Xia, Yong,Xiong, Ying,Song, Xue-Jiao,Lei, Qian,Peng, Cui-Ting,Tang, Hong,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
, p. 2764 - 2778 (2015)
The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16
Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models
Nguyen, William,Jacobson, Jonathan,Jarman, Kate E.,Jousset Sabroux, Helene,Harty, Leigh,McMahon, James,Lewin, Sharon R.,Purcell, Damian F.,Sleebs, Brad E.
, p. 5148 - 5175 (2019/05/28)
The persistent reservoir of cells latently infected with human immunodeficiency virus (HIV)-integrated proviral DNA necessitates lifelong suppressive antiretroviral therapy (ART). Epigenetic targeted compounds have shown promise as potential latency-reversing agents; however, these drugs have undesirable toxicity and lack specificity for HIV. We utilized a novel HEK293-derived FlpIn dual-reporter cell line, which quantifies specific HIV provirus reactivation (LTR promoter) relative to nonspecific host cell gene expression (CMV promoter), to identify the 5-substituted 2-acylaminothiazole hit class. Here, we describe the optimization of the hit class, defining the functionality necessary for HIV gene activation and for improving in vitro metabolism and solubility. The optimized compounds displayed enhanced HIV gene expression in HEK293 and Jurkat 10.6 latency cellular models and increased unspliced HIV RNA in resting CD4+ T cells isolated from HIV-infected individuals on ART, demonstrating the potential of the 2-acylaminothiazole class as latency-reversing agents.
ACTIVATORS OF HIV LATENCY
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Page/Page column 56, (2018/04/19)
The present invention relates to novel compounds which active HIV expression in latently infected cells. More particularly, the invention relates to pharmaceutical compositions comprising the novel compounds and their use in activating HIV expression in latently infected cells. Further still, the invention relates to pharmaceutical compositions comprising the novel compounds in combination with anti-HIV therapy compounds and their use in treating HIV infection in both animals and humans. The invention further provides means for preparing the compounds.
Imidazole [2, 1-b] thiazole derivative as well as preparation method and application thereof
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Paragraph 0137; 0138; 0139, (2017/01/02)
The invention belongs to the field of chemical pharmaceuticals, and particularly relates to an imidazole [2, 1-b] thiazole derivative as well as a preparation method and an application thereof. The structure of the imidazole [2, 1-b] thiazole derivative i
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication
Stachulski, Andrew V.,Pidathala, Chandrakala,Row, Eleanor C.,Sharma, Raman,Berry, Neil G.,Iqbal, Mazhar,Bentley, Joanne,Allman, Sarah A.,Edwards, Geoffrey,Helm, Alison,Hellier, Jennifer,Korba, Brent E.,Semple, J. Edward,Rossignol, Jean-Francois
supporting information; experimental part, p. 4119 - 4132 (2011/08/05)
We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-
BENZYL SUBSTITUTED TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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Page/Page column 58-59, (2010/12/29)
The invention provides triazine compounds and methods of their use to modulate protein kinases and to treat diseases mediated by said protein kinases.
TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
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Page/Page column 98, (2010/12/29)
Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.
IMIDAZO (1, 2-A) PYRIDINE COMPOUNDS AS VEGF-R2 INHIBITORS
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Page/Page column 23, (2008/06/13)
The present invention provides compounds that are inhibitors of VEGF-R2 of the formula: (I) and methods of using these compounds.
THIAZOLE-AMINE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS
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Page/Page column 28, (2008/06/13)
The present invention relates to compounds of the Formula (I) wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula (I) have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula (I).
2-AMINO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS
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Page/Page column 12, (2010/02/11)
Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1-C8 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1-C8 alkyl or C2-C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
