Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Potent and Selective Human β3-Adrenergic Receptor Agonists with Good Oral Bioavailability. Part I was written by Imanishi, Masashi;Tomishima, Yasuyo;Itou, Shinji;Hamashima, Hitoshi;Nakajima, Yutaka;Washizuka, Kenichi;Sakurai, Minoru;Matsui, Shigeo;Imamura, Emiko;Ueshima, Koji;Yamamoto, Takao;Yamamoto, Nobuhiro;Ishikawa, Hirofumi;Nakano, Keiko;Unami, Naoko;Hamada, Kaori;Matsumura, Yasuhiro;Takamura, Fujiko;Hattori, Kouji. And the article was included in Journal of Medicinal Chemistry in 2008.SDS of cas: 179232-29-2 This article mentions the following:
A novel class of biphenyl analogs containing a benzoic acid moiety based on lead compound I have been identified as potent and selective human β3 adrenergic receptor (β3-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal Ph ring of lead compound I, it has been discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, II and III were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds II and III were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β3-AR agonists. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2SDS of cas: 179232-29-2).
Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.SDS of cas: 179232-29-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary