Application In Synthesis of 6-Chlorobenzothiazol-2-ylamineOn May 1, 2020 ,《Discovery of 4-hydroxy-2-oxo-1,2-dihydroquinolines as potential inhibitors of Streptococcus pneumoniae, including drug-resistant strains》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Huddar, Srigouri; Park, Chul Min; Kim, Hyung Jun; Jang, Soojin; Lee, Sunkyung. The article conveys some information:
New therapies for treating drug-resistant pneumococcal infections are urgently needed. The novel scaffold 6-hydroxy-4-oxo-1,2-dihydro-4H-quinoline was shown to have similar efficacies against all three different serotypes of S. pneumoniae, ATCC 49617 (19F), ATCC BAA-1663 (15B), and ATCC 700904 (19A), in a resazurin-based high-throughput screen using the Korea Chem. Bank library. Further studies to identify a new lead with this scaffold, including tricyclic pyrrolo[3,2,1-ij]quinolone and pyrido[3,2,1-ij]quinolone derivatives, led to the identification of 6d, 7d and 12a. Compound 6d (IC50 = 0.92, 0.75, and 0.77μM), 7d (IC50 = 0.57, 0.66, and 0.38μM) and 12a() (IC50 = 0.27, 1.03, and 0.62μM) showed submicromolar IC50 values against 19F, 15B, and 19A, resp., and thus serve as a starting point for further optimization. While some of compounds in this series exhibited acceptable pharmacokinetic profiles in preliminary in vivo rat experiments, the most active compound 12a showed poor solubility and high plasma protein binding. Our current research efforts are focused on optimizing compounds to improve physicochem. properties as well as potency. The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Application In Synthesis of 6-Chlorobenzothiazol-2-ylamine)
6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Application In Synthesis of 6-Chlorobenzothiazol-2-ylamineThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica