3133-29-7Relevant articles and documents
Synthesis and anti-inflammatory activities of phloroglucinol-based derivatives
Li, Ning,Khan, Shabana I.,Qiu, Shi,Li, Xing-Cong
, (2018)
The natural product phloroglucinol-based derivatives representing monoacyl-, diacyl-, dimeric acyl-, alkylated monoacyl-, and the nitrogen-containing alkylated monoacylphloro- glucinols were synthesized and evaluated for inhibitory activities against the inflammatory mediators such as inducible nitric oxide synthase (iNOS) and nuclear factor kappaB (NF-κB). The diacylphloroglucinol compound 2 and the alkylated acylphloroglucinol compound 4 inhibited iNOS with IC50 values of 19.0 and 19.5 μM, respectively, and NF-κB with IC50 values of 34.0 and 37.5 μM, respectively. These compounds may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.
Diacylphloroglucinol derivatives as antioxidant agents: green synthesis, optimisation, in?vitro, and in silico evaluation
Prasetyo, Wahyu E.,Kusumaningsih, Triana,Firdaus, Maulidan,Marliana, Soerya D.,Suryanti, Venty,Artanti, Anif N.,Apriana, Ita,Anggraini, Septin D.
supporting information, (2021/03/06)
Several derivatives of diacylphloroglucinol (3a–3c and 5a–5b) as an analogue of natural product compound 2,4-diacetylphloroglucinol 3a, were successfully synthesised in an excellent yield via a greener Friedel–Craft acylation using methanesulfonic acid (MSA) as a catalyst under an ultrasound-assisted condition. Operational simplicity, excellent yield, expedient metal-free synthesis, energy-efficient and mild reaction conditions are the outstanding advantages in this procedure. A scaled-up reaction also revealed the practical suitability of this newly developed procedure. The effects of several process variables on 3a were carefully accomplished using response surface methodology (RSM). Moreover, the green credentials of the present protocol have been assessed using several established green metrics and compared to relevant procedures. Along with the monomers, dimeric diacylphloroglucinols (6a–6e) were also synthesised and their in?vitro antioxidant activity of these species were carried out. Furthermore, drug-likeness, density functional theory (DFT), and molecular docking studies were also established.
Discovery and Biomimetic Synthesis of a Phloroglucinol-Terpene Adduct Collection from Baeckea frutescens and Its Biogenetic Origin Insight
Luo, Shi-Lin,Hu, Li-Jun,Huang, Xiao-Jun,Su, Jun-Cheng,Shao, Xue-Hua,Wang, Lei,Xu, Han-Hong,Li, Chuang-Chuang,Wang, Ying,Ye, Wen-Cai
supporting information, p. 11104 - 11108 (2020/08/03)
A phloroglucinol-terpene adduct (PTA) collection consisting of twenty-four molecules featuring three skeletons was discovered from Baeckea frutescens. Inspired by its biosynthetic hypothesis, we synthesized this PTA collection by reductive activation of s
