Category: chlorides-buliding-blocksIn 2021 ,《Design, synthesis, in vitro determination and molecular docking studies of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl)pyridine derivatives with terminal sulfonamide derivatives in LPS-induced RAW264.7 macrophage cells》 was published in Medicinal Chemistry Research. The article was written by Mersal, Karim I.; Abdel-Maksoud, Mohammed S.; Ali, Eslam M. H.; Ammar, Usama M.; Zaraei, Seyed-Omar; Kim, Jae-Min; Kim, Su-Yeon; Lee, Kyung-Tae; Lee, Kwan Hyi; Kim, Si-Won; Park, Hyun-Mee; Ji, Mi-Jung; Oh, Chang-Hyun. The article contains the following contents:
In the present work, a new series of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl)pyridine possessing terminal Et or Pr sulfonamides I (R = H, F; n = 2,3; Ar = Ph, 4-FC6H4, 1-naphthyl, etc.) was designed and synthesized. The cytotoxic effect of the final compounds was measured by applying MTT assay in LPS-Induced RAW264.7 macrophage cells. The final target compounds were screened for their anti-inflammatory effect through their ability to inhibit NO and PGE2 production and cytokines production (TNF-α, IL-6, IL-1β) in LPS-induced RAW264.7 macrophage at 10μM concentration Compounds I (R = H; n = 3; Ar = 1-naphthyl), I (R = F; n = 3; Ar = 4-BrC6H4), and I (R = F; n = 3; Ar = 1-naphthyl) showed the highest inhibitory effect on NO production Compounds I (R = H, F; n = 3; Ar = 1-naphthyl) exhibited high PGE2 inhibition with IC50 values of 3.47, 2.54μM, resp. Compounds I (R = H, F; n = 3; Ar = 1-naphthyl) exhibited high cytokines inhibition >/= 60%. The most potent compounds I (R = H, F; n = 3; Ar = 1-naphthyl) were tested to determine their effect on iNOS and COX-2 mRNA expression level. Compound I (R = F; n = 3; Ar = 1-naphthyl) were activity on iNOS and COX-2 proteins level, pro-inflammatory mediators and cytokines was determined and showed remarkable inhibition for both proteins level. Compounds I (R = H, F; n = 3; Ar = 1-naphthyl) showed high binding affinity to COX-2 active site and exhibited similar binding interactions of the native ligand celecoxib. In addition to this study using 4-Chlorobenzenesulfonyl chloride, there are many other studies that have used 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Category: chlorides-buliding-blocks) was used in this study.
4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics