5-((3-Amidobenzyl)oxy)nicotinamides as Sirtuin 2 Inhibitors was written by Ai, Teng;Wilson, Daniel J.;More, Swati S.;Xie, Jiashu;Chen, Liqiang. And the article was included in Journal of Medicinal Chemistry in 2016.Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid This article mentions the following:
Derived from the previously reported human sirtuin 2 (SIRT2) inhibitors that were based on a 5-aminonaphthalen-1-yloxy nicotinamide core structure, 5-((3-amidobenzyl)oxy)nicotinamides offered excellent activity against SIRT2 and high isoenzyme selectivity over SIRT1 and SIRT3. Selected compounds also exhibited generally favorable in vitro absorption, distribution, metabolism, and excretion properties. Kinetic studies revealed that a representative SIRT2 inhibitor acted competitively against both NAD+ and the peptide substrate, an inhibitory modality that was supported by the computational study. More importantly, two selected compounds I and II exhibited significant protection against α-synuclein aggregation-induced cytotoxicity in SH-SY5Y cells. Therefore, 5-((3-amidobenzyl)oxy)nicotinamides represent a new class of SIRT2 inhibitors that are attractive candidates for further lead optimization in the continued effort to explore selective inhibition of SIRT2 as a potential therapy for Parkinson’s disease. In the experiment, the researchers used many compounds, for example, 4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid).
4-(4H-1,2,4-Triazol-4-yl)benzoic acid (cas: 157069-48-2) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Many triazoles have antifungal effects: the triazole antifungal drugs include fluconazole, isavuconazole, itraconazole, voriconazole, pramiconazole, ravuconazole, and posaconazole and triazole plant-protection fungicides include epoxiconazole, triadimenol, myclobutanil, propiconazole, prothioconazole, metconazole, cyproconazole, tebuconazole, flusilazole and paclobutrazol.Recommanded Product: 4-(4H-1,2,4-Triazol-4-yl)benzoic acid
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics