Amidoxime prodrugs convert to potent cell-active multimodal inhibitors of the dengue virus protease was written by Swarbrick, Crystall;Zogali, Vasiliki;Chan, Kitti Wing Ki;Kiousis, Dimitrios;Gwee, Chin Piaw;Wang, Sai;Lescar, Julien;Luo, Dahai;von Itzstein, Mark;Matsoukas, Minos-Timotheos;Panagiotakopoulos, George;Vasudevan, Subhash G.;Rassias, Gerasimos. And the article was included in European Journal of Medicinal Chemistry in 2021.Synthetic Route of C7H4ClF3O2S This article mentions the following:
The flavivirus genus of the Flaviviridae family comprises Dengue, Zika and West-Nile viruses which constitute unmet medical needs as neither appropriate antivirals nor safe vaccines are available. The dengue NS2BNS3 protease is one of the most promising validated targets for developing a dengue treatment however reported protease inhibitors suffer from toxicity and cellular inefficacy. Here we report SAR on our previously reported Zika-active carbazole scaffold, culminating in prodrug compound SP-471P (EC50 1.10μM, CC50 > 100μM) that generates SP-471 (I â?II); one of the most potent, non-cytotoxic and cell-active protease inhibitors described in the dengue literature. In cell-based assays, SP-471P leads to inhibition of viral RNA replication and complete abolishment of infective viral particle production even when administered 6 h post-infection. Mechanistically, SP-471 appears to inhibit both normal intermol. protease processes and intramol. cleavage events at the NS2BNS3 junction, as well as at NS3 internal sites, all critical for virus replication. These render SP-471 a unique to date multimodal inhibitor of the dengue protease. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Synthetic Route of C7H4ClF3O2S).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Synthetic Route of C7H4ClF3O2S
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics