Cross, R. Matthew published the artcileOrally Bioavailable 6-Chloro-7-methoxy-4(1H)-quinolones Efficacious against Multiple Stages of Plasmodium, COA of Formula: C5H6BNO2, the publication is Journal of Medicinal Chemistry (2014), 57(21), 8860-8879, database is CAplus and MEDLINE.
The continued proliferation of malaria throughout temperate and tropical regions of the world has promoted a push for more efficacious treatments to combat the disease. Unfortunately, more recent remedies such as artemisinin combination therapies have been rendered less effective due to developing parasite resistance, and new drugs are required that target the parasite in the liver to support the disease elimination efforts. Research was initiated to revisit antimalarials developed in the 1940s and 1960s that were deemed unsuitable for use as therapeutic agents as a result of poor understanding of both physicochem. properties and parasitol. Structure-activity and structure-property relationship studies were conducted to generate a set of compounds with the general 6-chloro-7-methoxy-2-methyl-4(1H)-quinolone scaffold which were substituted at the 3-position with a variety of Ph moieties possessing various properties. Extensive physicochem. evaluation of the quinolone series was carried out to down-select the most promising 4(1H)-quinolones, P4Q-391 (7), 6-Chloro-7-methoxy-2-methyl-3-(2-methyl-4-(4(trifluoromethoxy)phenoxy)phenyl)-quinolin-4(1H)-one (62), 6-Chloro-3-(6-(2-fluoro-4-(trifluoromethyl)phenyl)pyridin-3-yl)-7-methoxy-2-methylquinolin-4(1H)-one (66), and 6-Chloro-7-methoxy-2-methyl-3-(6-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)quinolin-4(1H)-one(67), which possessed low-nanomolar EC50 values against W2 and TM90-C2B as well as improved microsomal stability. Addnl., in vivo Thompson test results using Plasmodium berghei in mice showed that these 4(1H)-quinolones were efficacious for the reduction of parasitemia at >99% after 6 days.
Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, COA of Formula: C5H6BNO2.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem