Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization was written by Fulp, Jacob;He, Liu;Toldo, Stefano;Jiang, Yuqi;Boice, Ashley;Guo, Chunqing;Li, Xia;Rolfe, Andrew;Sun, Dong;Abbate, Antonio;Wang, Xiang-Yang;Zhang, Shijun. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C8H7ClO3 This article mentions the following:
NLRP3 inflammasome plays critical roles in a variety of human diseases and represents a promising drug target. In this study, we established the in vivo functional activities of JC124, a previously identified NLRP3 inflammasome inhibitor from our group, in mouse models of Alzheimer’s disease and acute myocardial infarction. To understand the chem. space of this lead structure, a series of analogs were designed, synthesized, and biol. characterized. The results revealed the critical roles of the two substituents on the benzamide moiety of JC124. On the other hand, modifications on the sulfonamide moiety of JC124 are well tolerated. Two new lead compounds, 14 and 17, were identified with improved inhibitory potency (IC50 values of 0.55 ± 0.091 and 0.42 ± 0.080 μM, resp.). Further characterization confirmed their selectivity and in vivo target engagement. Collectively, the results strongly encourage further development of more potent analogs based on this chem. scaffold. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2COA of Formula: C8H7ClO3).
5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.COA of Formula: C8H7ClO3
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics