《Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 1》 was written by Kirk, R.; Ratcliffe, A.; Noonan, G.; Uosis-Martin, M.; Lyth, D.; Bardell-Cox, O.; Massam, J.; Schofield, P.; Hindley, S.; Jones, D. R.; Maclean, J.; Smith, A.; Savage, V.; Mohmed, S.; Charrier, C.; Salisbury, A-M.; Moyo, E.; Metzger, R.; Chalam-Judge, N.; Cheung, J.; Stokes, N. R.; Best, S.; Craighead, M.; Armer, R.; Huxley, A.. Recommanded Product: 6-Bromopyridin-3-amineThis research focused ontricyclic topoisomerase inhibitor bacterial infection treatment. The article conveys some information:
The alarming reduction in drug effectiveness against bacterial infections has created an urgent need for the development of new antibacterial agents that circumvent bacterial resistance mechanisms. We report here a series of DNA gyrase and topoisomerase IV inhibitors that demonstrate potent activity against a range of Gram-pos. and selected Gram-neg. organisms, including clin.-relevant and drug-resistant strains. In part 1, we present a detailed structure activity relationship (SAR) anal. that led to the discovery of our previously disclosed compound, REDX05931, which has a min. inhibitory concentration (MIC) of 0.06 μg mL-1 against fluoroquinolone-resistant Staphylococcus aureus. Although in vitro hERG and CYP inhibition precluded further development, it validates a rational design approach to address this urgent unmet medical need and provides a scaffold for further optimization, which is presented in part 2. The experimental part of the paper was very detailed, including the reaction process of 6-Bromopyridin-3-amine(cas: 13534-97-9Recommanded Product: 6-Bromopyridin-3-amine)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Recommanded Product: 6-Bromopyridin-3-amine