On March 10, 2016, Abraham, Rebecca J.; Stevens, Andrew J.; Young, Kelly A.; Russell, Cecilia; Qvist, Anastasia; Khazandi, Manouchehr; Wong, Hui San; Abraham, Sam; Ogunniyi, Abiodun D.; Page, Stephen W.; O’Handley, Ryan; McCluskey, Adam; Trott, Darren J. published an article.Formula: C9H5ClOS The title of the article was Robenidine Analogues as Gram-Positive Antibacterial Agents. And the article contained the following:
Robenidine, (2,2′-bis[(4-chlorophenyl)methylene]carbonimidic dihydrazide) (1), was active against MRSA and VRE with MIC’s of 8.1 and 4.7 μM, resp. SAR revealed tolerance for 4-Cl isosteres, and imine carbon alkylation identified a methyl/ethyl binding pocket that also accommodated a CH2OH moiety. Other analigs were active against 24 clin. MRSA and MSSA isolates, and no dose-limiting cytotoxicity at ≥2× MIC or hemolysis at ≥8× MIC was observed Polymyxin B addition engendered Escherichia coli and Pseudomonas aeruginosa Gram-neg. activity MIC’s of 4.2-21.6 μM. 1 and 75 displayed excellent microsomal stability, intrinsic clearance, and hepatic extraction ratios with T1/2 > 247 min, CLint < 7 μL/min/mg protein, and EH < 0.22 in both human and mouse liposomes for 1 and in human liposomes for I. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Formula: C9H5ClOS
The Article related to robenidine antibacterial bacterial infection, Pharmacology: Structure-Activity and other aspects.Formula: C9H5ClOS
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem