Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. Part 2. Identification and Structure-Activity Relationships of a Novel Series of N-Alkyl-N-(heteroaryl-substituted benzyl)-N’-arylureas was written by Tanaka, Akira;Terasawa, Takeshi;Hagihara, Hiroyuki;Sakuma, Yuri;Ishibe, Noriko;Sawada, Masae;Takasugi, Hisashi;Tanaka, Hirokazu. And the article was included in Journal of Medicinal Chemistry in 1998.HPLC of Formula: 179056-04-3 This article mentions the following:
A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N’-arylurea and related derivatives have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. A pyrazol-3-yl group on the N-benzyl group was identified as a heteroaromatic ring providing a good profile of biol. activity. As a result of optimization of the combination with the N-alkyl group and N-aryl group, compound FR186054 was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irresp. of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicol. study revealed this compound to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po. In the experiment, the researchers used many compounds, for example, 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3HPLC of Formula: 179056-04-3).
4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules.HPLC of Formula: 179056-04-3
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics