Identification of a Novel 1,2,3,4-Tetrahydrobenzo[b][1,6]naphthyridine Analogue as a Potent Phosphodiesterase 5 Inhibitor with Improved Aqueous Solubility for the Treatment of Alzheimer’s Disease was written by Fiorito, Jole;Vendome, Jeremie;Saeed, Faisal;Staniszewski, Agnieszka;Zhang, Hong;Yan, Shijun;Deng, Shi-Xian;Arancio, Ottavio;Landry, Donald W.. And the article was included in Journal of Medicinal Chemistry in 2017.COA of Formula: C7H13NO This article mentions the following:
Phosphodiesterase 5 (PDE5) hydrolyzes cGMP leading to increased levels of the cAMP response element binding protein (CREB), a transcriptional factor involved with learning and memory processes. The authors previously reported potent quinoline-based PDE5 inhibitors (PDE5Is) for the treatment of Alzheimer’s disease (AD). However, the low aqueous solubility rendered them undesirable drug candidates. Here the authors report a series of novel PDE5Is with two new scaffolds, 1,2,3,4-tetrahydrobenzo[b][1,6]naphthyridine and 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one. Among them, compound I, the most potent compound, has an excellent in vitro IC50 (0.056 nM) and improved aqueous solubility as well as good efficacy in a mouse model of AD. Furthermore, the authors are proposing two plausible binding modes obtained through in silico docking, which provide insights into the structural basis of the activity of the two series of compounds reported herein. In the experiment, the researchers used many compounds, for example, 1-Ethylpiperidin-4-one (cas: 3612-18-8COA of Formula: C7H13NO).
1-Ethylpiperidin-4-one (cas: 3612-18-8) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.COA of Formula: C7H13NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem