Anti-biofilm Agents against Pseudomonas aeruginosa: A Structure-Activity Relationship Study of C-Glycosidic LecB Inhibitors was written by Sommer, Roman;Rox, Katharina;Wagner, Stefanie;Hauck, Dirk;Henrikus, Sarah S.;Newsad, Shelby;Arnold, Tatjana;Ryckmans, Thomas;Broenstrup, Mark;Imberty, Anne;Varrot, Annabelle;Hartmann, Rolf W.;Titz, Alexander. And the article was included in Journal of Medicinal Chemistry in 2019.Related Products of 69815-97-0 This article mentions the following:
Biofilm formation is a key mechanism of antimicrobial resistance. We have recently reported two classes of orally bioavailable C-glycosidic inhibitors of the Pseudomonas aeruginosa lectin LecB with antibiofilm activity. They proved efficient in target binding, were metabolically stable, nontoxic, selective, and potent in inhibiting formation of bacterial biofilm. Here, we designed and synthesized six new carboxamides and 24 new sulfonamides for a detailed structure-activity relationship for two clin. representative LecB variants. Sulfonamides generally showed higher inhibition compared to carboxamides, which was rationalized based on crystal structure analyses. Substitutions at the thiophenesulfonamide increased binding through extensive contacts with a lipophilic protein patch. These metabolically stable compounds showed a further increase in potency toward the target and in biofilm inhibition assays. In general, we established the structure-activity relationship for these promising antibiofilm agents and showed that modification of the sulfonamide residue bears future optimization potential. In the experiment, the researchers used many compounds, for example, 4-Methylthiophene-2-sulfonyl chloride (cas: 69815-97-0Related Products of 69815-97-0).
4-Methylthiophene-2-sulfonyl chloride (cas: 69815-97-0) belongs to benzothiophene derivatives. Benzothiophene scaffolds are of great importance due to its increased presence in bioactive molecules. It is found within the chemical structures of pharmaceutical drugs such as raloxifene, zileuton, sertaconazole, and also BTCP.Related Products of 69815-97-0
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem