Quality Control of 4-Methoxybenzaldehyde. In 2021 EUR J MED CHEM published article about PHASE-II TRIAL; CARBOXYLESTERASE ISOZYMES; DERIVATIVES; PROBE; IRINOTECAN; LOPERAMIDE; DISCOVERY; SUBSTRATE; PROGRESS in [Huo, Peng-Chao; Guan, Xiao-Qing; Song, Yun-Qing; Sun, Meng-Ru; He, Rong-Jing; Zou, Li-Wei; Xue, Li-Juan; Shi, Jin-Hui; Ge, Guang-Bo] Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Integrat Med Res, Shanghai, Peoples R China; [Huo, Peng-Chao; Zhang, Nan] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China; [Liu, Peng; Liu, Zhi-Guo] Wenzhou Med Univ, Chem Biol Res Ctr, Sch Pharmaceut Sci, Wenzhou, Zhejiang, Peoples R China in 2021, Cited 36. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5.
Human carboxylesterase 2 (hCES2A), one of the major serine hydrolases distributed in the small intestine, plays a crucial role in hydrolysis of ester-bearing drugs. Accumulating evidence has indicated that hCES2A inhibitor therapy can modulate the pharmacokinetic and toxicological profiles of some important hCES2A-substrate drugs, such as the anticancer agent CPT-11. Herein, a series of indanone-chalcone hybrids are designed and synthesized to find potent and highly selective hCES2A inhibitors. Inhibition assays demonstrated that most indanone-chalcone hybrids displayed strong to moderate hCES2A inhibition activities. Structure-hCES2A inhibition activity relationship studies showed that introduction of a hydroxyl at the C4′ site and introduction of an N-alkyl group at the C6 site were beneficial for hCES2A inhibition. Particularly, B7 (an N-alkylated 1-indanoneechalcone hybrid) exhibited the most potent inhibition on hCES2A and excellent specificity (this agent could not inhibit other human esterases including hCES1A and butyrylcholinesterase). Inhibition kinetic analyses demonstrated that B7 potently inhibited hCES2A-mediated FD hydrolysis in a mixed inhibition manner, with a calculated K-i value of 0.068 mu M. Furthermore, B7 was capable of inhibiting intracellular hCES2A in living cells and displayed good metabolic stability. Collectively, our findings show that indanone-chalcone hybrids are good choices for the development of hCES2A inhibitors, while B7 is a promising candidate for the development of novel anti-diarrhea agents to ameliorate irinotecan-induced intestinal toxicity. (c) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
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