N-Phenyl indole derivatives as AT1 antagonists with anti-hypertension activities: Design, synthesis and biological evaluation was written by Zhu, Weibo;Bao, Xiaolu;Ren, He;Da, Yajing;Wu, Dan;Li, Fuming;Yan, Yijia;Wang, Li;Chen, Zhilong. And the article was included in European Journal of Medicinal Chemistry in 2016.HPLC of Formula: 4373-61-9 This article mentions the following:
The design, synthesis, in vitro and in vivo evaluation of 6-substituted benzimidazole with 1, 4-disubstituted or 1, 5-disubstituted indole derivatives as novel angiotensin II receptor antagonists are outlined. Radioligand binding assays showed that several 6-substituted benzimidazole derivatives displayed high affinities binding to the angiotensin II type 1 receptor at the same order of magnitude to telmisartan. The biol. evaluation on spontaneously hypertensive rats showed that 2-[4-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazole-1-yl]methyl]-1H-indol-1-yl]benzoic acid, I, could cause significant decrease on MBP in a dose dependent manner. Its maximal response lowered 53 mmHg of MBP at 5 mg/kg and 64 mmHg of MBP at 10 mg/kg after oral administration, and the significant antihypertensive effect lasted beyond 24 h, which was better than both losartan and telmisartan. A study designed to determine acute toxicity showed that I had low acute toxicity with no significant changes in the weight and no obvious untoward reactions. The encouraging results make I an effective and durable anti-hypertension drug candidate and deserve further investigation for therapeutic application. In the experiment, the researchers used many compounds, for example, 2-(m-Tolyl)pyridine (cas: 4373-61-9HPLC of Formula: 4373-61-9).
2-(m-Tolyl)pyridine (cas: 4373-61-9) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the 锜?bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the 锜?bonds. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.HPLC of Formula: 4373-61-9