Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists was written by Liu, Peng;Xu, Xing;Chen, Lili;Ma, Lei;Shen, Xu;Hu, Lihong. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Name: 1-Bromo-6-chlorohexane The following contents are mentioned in the article:
Compound I [R = HO] (IC50 = 35.2±7.2 μM), a moderate FXR antagonist was discovered via high-throughput screening. Structure-activity relationship studies indicated that the shape and the lipophilicity of the substituents of the aromatic ring affect the activity dramatically, increasing the shape and the lipophilicity of the substituents of the aromatic ring enhances the potency of FXR antagonists. Especially, when the OH at C2 position of the aromatic ring was replaced by the BnO substituent (analog I [R = PhCH2O]), its activity could be improved to IC50 = 1.1±0.1 μM. Besides, the length of the linker and the tetrazole structure are essential for retaining the activity. This study involved multiple reactions and reactants, such as 1-Bromo-6-chlorohexane (cas: 6294-17-3Name: 1-Bromo-6-chlorohexane).
1-Bromo-6-chlorohexane (cas: 6294-17-3) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Name: 1-Bromo-6-chlorohexane
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics