Wilson, Colin R. published the artcileNovel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, the publication is Journal of Medicinal Chemistry (2017), 60(24), 10118-10134, database is CAplus and MEDLINE.
A BioFocus DPI SoftFocus library of ∼35,000 compounds was screened against Mycobacterium tuberculosis (Mtb) to identify novel hits with antitubercular activity. The hits were evaluated in biol. triage assays to exclude compounds suggested to function via frequently encountered promiscuous mechanisms of action including inhibition of the QcrB subunit of the cytochrome bc1 complex, disruption of cell-wall homeostasis, and DNA damage. Among the hits that passed this screening cascade, a 6-dialkylaminopyrimidine carboxamide series was prioritized for hit to lead optimization. Compounds from this series were active against clin. Mtb strains, while no cross-resistance to conventional antituberculosis drugs was observed This suggested a novel mechanism of action, which was confirmed by chemoproteomic anal. leading to the identification of BCG_3193 and BCG_3827 as putative targets of the series with unknown function. Initial structure-activity relationship studies have resulted in compounds with moderate to potent antitubercular activity and improved physicochem. properties.
Journal of Medicinal Chemistry published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H4BrF10N, Recommanded Product: 6-(4-Methylpiperazin-1-yl)pyridin-3-amine.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics