Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment was written by Shu, Min;Loebach, Jennifer L.;Parker, Kerry A.;Mills, Sander G.;Chapman, Kevin T.;Shen, Dong-Ming;Malkowitz, Lorraine;Springer, Martin S.;Gould, Sandra L.;DeMartino, Julie A.;Siciliano, Salvatore J.;Di Salvo, Jerry;Lyons, Kathy;Pivnichny, James V.;Kwei, Gloria Y.;Carella, Anthony;Carver, Gwen;Holmes, Karen;Schleif, William A.;Danzeisen, Renee;Hazuda, Daria;Kessler, Joseph;Lineberger, Janet;Miller, Michael D.;Emini, Emilio A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2004.SDS of cas: 6834-42-0 This article mentions the following:
Extensive SAR studies in our benzylpyrazole series of CCR5 antagonists have shown that both lipophilic and hydrophilic substituents on the Ph of the benzyl group increase antiviral potency. However, improvements in pharmacokinetic profiles were generally only observed with more lipophilic substitutions. 4-Biphenyl performed the best in this regard. Highly lipophilic substituents impart undesirable ion channel activity to these CCR5 antagonists. Alkoxy substituents provide a good balance of antiviral activity, pharmacokinetic parameters, and selectivity. Compounds containing a 3,4-dimethoxy substituent, are considered the most promising improvements over parent compounds They demonstrate improved antiviral activity while retaining good pharmacokinetic profile and selectivity. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0SDS of cas: 6834-42-0).
2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.SDS of cas: 6834-42-0
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics