Mederski, WWKR published the artcileNovel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridines. Potent angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes, Product Details of C7H5Br2F, the publication is European Journal of Medicinal Chemistry (1997), 32(6), 479-491, database is CAplus.
The synthesis and pharmacol. activity of balanced high affinity non-peptide angiotensin II antagonists of the AT1 and AT2 subtype receptors have been presented. A series of previously prepared AT1 selective 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]-pyridines were modified at four different positions in order to increase the AT2 binding affinity by maintaining the nanomolar activity for the AT1 receptor. The targeted AT2/AT1 IC50 binding ratio of ∼ 1 was achieved with a number of compounds possessing a small alkyl chain at C-2, different acetamide groups at N-5 and a 3-fluoro and 2′-carboxamidosulfonyl substituent at the biphenylmethyl moiety. These modifications led to an analog which exhibited an AT2/AT1 ratio of 0.74, a subnanomolar AT1 antagonistic potency (0.18 nM) and a high metabolic stability in rat and monkey liver microsomes in vitro. After oral administration of 3 mg/kg to cynomolgus monkeys, EMD 90423 (potassium salt of the active analog) demonstrated good efficacy and a long duration of action as an antihypertensive agent.
European 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, Product Details of C7H5Br2F.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary