749204-15-7Relevant academic research and scientific papers
Discovery of aminothiazole derivatives as novel human enterovirus A71 capsid protein inhibitors
Cai, Yang,Chen, Yinuo,Dong, Chune,Lan, Ke,Lei, Ping,Tang, Qi,Wu, Shuwen,Xu, Ting,Xu, Zhichao,Zhou, Hai-Bing,Zou, Wenting
, (2022/03/15)
Enterovirus A71 (EV-A71), one of the major pathogens that causes hand, foot and mouth disease (HFMD), has seriously threatened the health and safety of young children. In this study, aminothiazole derivatives were synthesized and screened against EV-A71 in Rhabdomyosarcoma (RD) cells. The best compound (12s), with a biphenyl group, showed activity against EV-A71 (EC50: 0.27 μM) but also against a series of different human enteroviruses without significant cytotoxicity (CC50 > 56.2 μM). Mechanistic studies including time-of-drug-addition assays, viral entry assays and microscale thermophoresis (MST) experiments, showed that 12s binds to EV-A71 capsid and blocks the binding between the viral protein VP1 and the relevant human scavenger receptor class B member 2 (hSCARB2).
Novel imidazopyrimidines-based molecules induce tetramerization of tumor pyruvate kinase M2 and exhibit potent antiproliferative profile
Patel, Sagarkumar,Globisch, Christoph,Pulugu, Priyanka,Kumar, Prasoon,Jain, Alok,Shard, Amit
, (2022/01/11)
Discovery of novel and potent lead molecules for the specific therapeutic targets by de novo drug design is still in infancy. Here, we disclose the unprecedented development of imidazopyri(mi)dine-based tumor pyruvate kinase M2 (PKM2) modulators by subseq
Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease
Sagar, Sneha R.,Singh, Devendra Pratap,Das, Rajesh D.,Panchal, Nirupa B.,Sudarsanam, Vasudevan,Nivsarkar, Manish,Vasu, Kamala K.
, (2021/03/06)
Alzheimer's disease (AD) is a neurodegenerative disease majorly affecting old age populations. Various factors that affect the progression of the disease include, amyloid plaque formation, neurofibrillary tangles, inflammation, oxidative stress, etc. Here
Imidazo[1,2-a]pyridines linked with thiazoles/thiophene motif through keto spacer as potential cytotoxic agents and NF-κB inhibitors
Vasu, Kamala K.,Digwal, Chander Singh,Pandya, Amit N.,Pandya, Dhaivat H.,Sharma, Jayesh A.,Patel, Sneha,Agarwal, Milee
supporting information, p. 5463 - 5466 (2017/11/17)
A series of new imidazo[1,2-a]pyridine linked with thiazole/thiophene motif through a keto spacer were synthesized and tested for their cytotoxic potential against three human cancer cell lines including A549, HeLa and U87-MG using MTT assay. Compounds A2
A revised approach to the synthesis of 3-acyl imidazo[l,2-a] pyridines
Gomez, Omar,Salgado-Zamora, Hector,Reyes, Alicia,Campos, Maria Elena
experimental part, p. 99 - 103 (2011/06/27)
3-Acyl imidazo[l,2-a]pyridines with no substituent at position 2 were obtained in moderate to good yields in an improved version of the Tisler protocol for the synthesis of imidazo[l,2-x]azines. It was found that yields are significantly improved if the r
