In 2020 EUR J MED CHEM published article about BIOLOGICAL EVALUATION; AMPK; ADIPOGENESIS/LIPOGENESIS; DERIVATIVES; INHIBITORS; DESIGN; MICE in [Rao, Yong; Xu, Zhao; Hu, Yu-Tao; Li, Chan; Xu, Yao-Hao; Song, Qin-Qin; Yu, Hong; Song, Bing-Bing; Chen, Shuo-Bin; Li, Qing-Jiang; Huang, Shi-Liang; Tan, Jia-Heng; Ou, Tian-Miao; Wang, Hong-Gen; Huang, Zhi-Shu] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangdong Prov Key Lab New Drug Design & Evaluat, Guangzhou 510006, Guangdong, Peoples R China; [Ye, Ji-Ming] RMIT Univ, Sch Hlth & Biomed Sci, Mol Pharmacol Diabet Grp, Melbourne, Vic 3083, Australia; [Zhong, Guo-Ping] Sun Yat Sen Univ, Sch Pharmaceut Sci, Lab Drug Metab & Pharmacokinet, Guangzhou, Peoples R China in 2020, Cited 34. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Name: 2-Aminobenzamide
Discovery of novel anti-obesity agents is a challenging and promising research area. Based on our previous works, we synthesized 40 novel beta-indoloquinazoline analogues by altering the skeleton and introducing preferential side chains, evaluated their lipid-lowering activity and summarized the structure-activity relationships. In combination with an evaluation of the lipid-lowering efficacies, AMP-dependent activated protein kinase (AMPK) activating ability and liver microsomal stability, compound 23 (named as IQZ23) was selected for further studies. IQZ23 exerted a high efficacy in decreasing the triglyceride level (EC50 = 0.033 mu M) in 3T3-L1 adipocytes. Mechanistic studies revealed the lipid-lowering activity of IQZ23 was dependent on the AMPK pathway by modulating ATP synthase activity. This activation was accompanied by mitochondrial biogenesis and oxidation capacity increased, and insulin sensitivity enhanced in pertinent cell models by various interventions. Correspondingly, IQZ23 (20 mg/kg, i.p.) treatment significantly reversed high fat and cholesterol diet (HFC)- induced body weight increases and accompanying clinical symptoms of obesity in mice but without indicative toxicity. These results indicate that IQZ23 could be a useful candidate for the treatment of obesity and related metabolic disorders. (c) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem