Ontology highlight
ABSTRACT:
SUBMITTER: Jiang Y
PROVIDER: S-EPMC6856409 | biostudies-literature | 2019 Nov
REPOSITORIES: biostudies-literature
Jiang Yuqi Y He Liu L Green Jakob J Blevins Hallie H Guo Chunqing C Patel Sulay Harsiddhbhai SH Halquist Matthew S MS McRae MaryPeace M Venitz Jürgen J Wang Xiang-Yang XY Zhang Shijun S
Journal of medicinal chemistry 20191031 21
NLRP3 inflammasomes have recently emerged as an attractive drug target for neurodegenerative disorders. In our continuing studies, a new chemical scaffold was designed as selective inhibitors of NLRP3 inflammasomes. Initial characterization of the lead <b>HL16</b> demonstrated improved, however, nonselective inhibition on the NLRP3 inflammasome. Structure-activity relationship studies of <b>HL16</b> identified a new lead, <b>17</b> (<b>YQ128</b>), with an IC<sub>50</sub> of 0.30 ± 0.01 μM. Furth ...[more]