Development of indole-2-carbonyl piperazine urea derivatives as selective FAAH inhibitors for efficient treatment of depression and pain was written by Shang, Yanguo;Wang, Minghui;Hao, Qingjing;Meng, Tao;Li, Lili;Shi, Junwei;Yang, Guoqing;Zhang, Zhilan;Yang, Kan;Wang, Jinxin. And the article was included in Bioorganic Chemistry in 2022.Formula: C9H6ClNO2 This article mentions the following:
Fatty acid amide hydrolase (FAAH), a serine hydrolase with significant role in the hydrolysis of endocannabinoids, is a promising therapeutic target for peripheral and central nervous system related disorders, including pain, neuroinflammation and depression. Employing a structure-based approach, a novel series of indole-2-carbonyl piperazine urea derivatives were designed and synthesized as FAAH inhibitors for the treatment of pain-depression comorbidity. Among them, compound 4i emerged as the most potent inhibitor (IC50 = 0.12 μM) with fine selectivity vs. CES2, ABHD6, MAGL and the cannabinoid receptor, which also displayed superior metabolic stability in human liver microsome and an adequate pharmacokinetic profile in rodents. Treatment of depressed rats with 4i demonstrated favorable antidepressant-like effects not only by increasing the level of BDNF in the hippocampus but also by restraining the apoptosis of hippocampal neurons. Also, 4i effectively suppressed the LPS-induced neuroinflammation in vitro. Moreover, 4i exhibited potent analgesic activity, which indicated its promising therapeutical application for pain and depression. These meaningful results shed light on FAAH inhibitors as promising pain-depression comorbidity therapeutics. In the experiment, the researchers used many compounds, for example, 6-Chloroindole-2-carboxylic acid (cas: 16732-75-5Formula: C9H6ClNO2).
6-Chloroindole-2-carboxylic acid (cas: 16732-75-5) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C9H6ClNO2
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles