Fan, Tian-Yun published the artcileSynthesis and antibacterial evaluation of 13-substituted cycloberberine derivatives as a novel class of anti-MRSA agents, Safety of (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, the publication is European Journal of Medicinal Chemistry (2018), 877-886, database is CAplus and MEDLINE.
A series of new 13-substituted cycloberberine (CBBR) derivatives I [R = H, 2-Me, 4-iso-Pr, 3′,5′-(CF3)2, etc.], II (R = 3′-pyridyl, 4′-pyridyl), and III (R = Me, CO2Me) were prepared and evaluated for their antibacterial activities against Gram-pos. bacteria taking CBBR as the lead. Structure-activity relationship revealed that the introduction of a suitable electron-donating group at the 13-position in CBBR might be beneficial for the antibacterial potency. Among them, compounds I (R = 2-Me) (IV) and III (R = Me) exhibited high potency against methicillin-sensitive (MSSA) and resistant strains of S. aureus (MRSA) with MIC values of 1-4 μg/mL. Both of them also displayed high stabilities in blood, and good in vivo safety profiles with LD50 values of 65.6 and 41.2 mg kg-1 in i.v. route, resp. Mol. docking anal. indicated that compound IV might target FtsZ protein that could inhibit cell division, with the advantage of activity against multidrug resistant S. aureus. Therefore, we consider 13-substituted CBBR derivatives to be a novel class of anti-MRSA agents worthy of further investigation.
European Journal of Medicinal Chemistry published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Safety of (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary