Malamas, Michael S. published the artcileDesign and Structure-Activity Relationships of Isothiocyanates as Potent and Selective N-Acylethanolamine-Hydrolyzing Acid Amidase Inhibitors, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5956-5972, database is CAplus and MEDLINE.
N-Acylethanolamines are signaling lipid mols. implicated in pathophysiol. conditions associated with inflammation and pain. N-Acylethanolamine acid amidase (NAAA) favorably hydrolyzes lipid palmitoylethanolamide, which plays a key role in the regulation of inflammatory and pain processes. The synthesis and structure-activity relationship studies encompassing the isothiocyanate pharmacophore have produced potent low nanomolar inhibitors for hNAAA, while exhibiting high selectivity (>100-fold) against other serine hydrolases and cysteine peptidases. We have followed a target-based structure-activity relationship approach, supported by computational methods and known cocrystals of hNAAA. We have identified systemically active inhibitors with good plasma stability (t1/2 > 2 h) and microsomal stability (t1/2 ∼ 15-30 min) as pharmacol. tools to investigate the role of NAAA in inflammation, pain, and drug addiction.
Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary