Picard, Franck published the artcileSynthesis and Evaluation of 2′-Substituted 4-(4′-Carboxy- or 4′-carboxymethylbenzylidene)-N-acylpiperidines: Highly Potent and in Vivo Active Steroid 5α-Reductase Type 2 Inhibitors, Formula: C7H5Br2F, the publication is Journal of Medicinal Chemistry (2002), 45(16), 3406-3417, database is CAplus and MEDLINE.
Sixteen N-acylpiperidines I (R1 = Ph2CH, Ph2CHCH2, dicyclohexylmethyl, 1-adamantyl; R2 = H, F, MeO; R3 = H, HO2C; R4 = H, HO2C, HO2CCH2) and II (R5 = Ph2CH, Ph2N, Me3CO, 1-adamantyl), bearing carboxylic acid moieties, were synthesized and evaluated for inhibition of rat and human steroid 5α-reductase isoenzymes types 1 and 2. In the dicyclohexylacetyl series (R1 = dicyclohexylmethyl), fluorination in the 2-position of the benzene nucleus, exchange of the carboxy group by a carboxymethyl moiety, and combination of both structural modifications led to highly active inhibitors of the human type 2 isoenzyme [IC50 values: I [R2 = F, R3 = H, R4 = HO2C; (III)], 11 nM; I (R2 = R3 = H, R4 = HO2CCH2), 6 nM; I (R2 = F, R3 = H, R4 = HO2CCH2), 7 nM; finasteride, 5 nM]. In vivo all compounds tested markedly reduced the prostate weights in castrated testosterone-treated rats. Oral activity was shown for compound I (R1 = dicyclohexylmethyl, R2 = R3 = H, R4 = HO2C). From the finding that III is active in the rat, although it is a rather poor inhibitor of the rat enzyme and is a strong inhibitor of the human enzyme, it is concluded that it should be highly potent in men.
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, Formula: C7H5Br2F.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary