82195-61-7Relevant academic research and scientific papers
Structure-activity relationship studies of (E)-3,4-dihydroxystyryl alkyl sulfones as novel neuroprotective agents based on improved antioxidant, anti-inflammatory activities and BBB permeability
Chen, Ying,Wu, Bolin,Hao, Yameng,Liu, Yunqi,Zhang, Zhili,Tian, Chao,Ning, Xianling,Guo, Ying,Liu, Junyi,Wang, Xiaowei
, p. 420 - 433 (2019/03/29)
(E)-3,4-dihydroxystyryl alkyl sulfones, as new analogues of neurodegenerative agents, were designed and synthesized. The biological results demonstrated that most of the target compounds preserved antioxidant and anti-inflammatory potency in scavenging reactive free radicals, protecting neuronal cells against neurotoxins such as H2O2, 6-hydroxydopamine and inhibiting lipopolysaccharide (LPS)-induced over-production of NO. Among these compounds, 6.22 with cyclopentyl propyl exhibited prominent antioxidant activity at low concentration (2.5 μM) in H2O2 model (cell viability = 94.5%). In addition, 6.22 (IC50 = 1.6 μM) displayed better anti-inflammatory activity than that of lead compound 1 (IC50 = 13.4 μM). In view of the outstanding performance of 6.22, the apoptotic rates of H2O2-damaged PC12 cells were detected by Annexin V-FITC/PI assay. 6.22 showed higher potency in inhibition of apoptosis than 1 at low concentration (2.5 μM), consisting with the antioxidant and anti-inflammatory models. Furthermore, with the predicted CNS (+) blood-brain barrier (BBB) permeability (Pe = 6.84 × 10?6 cm s?1), low cytotoxicity and favorable physiochemical properties based on calculation, compound 6.22 can be further developed as a potential multifunctional neuroprotective agent.
SILICON IN ORGANIC SYNTHESIS-17 CYCLOPENTANNULATION BY THERMOLYSIS OF (1-TRIMETHYLSILYLCYCLOPROPYL)ETHYLENES-THE 1-TRIMETHYLSILYLCYCLOPROPYL ANION
Paquette, Leo A.,Wells, Gregory J.,Horn, Keith A.,Yan, Tu-Hsin
, p. 913 - 924 (2007/10/02)
Several alternatives for preparing (1-trimethylsilylcyclopropyl)ethylenes have been examined.Although 1-lithio-1-(trimethylsilyl)ethylene does add satisfactorily to carbonyl compounds and the subsequent Simmons-Smith cyclopropanation provides the desired
SILICON IN ORGANIC SYNTHESIS. 13. THE 1-TRIMETHYLSILYLCYCLOPROPYL ANION AND ITS FORMAL EQUIVALENT
Paquette, Leo A.,Horn, Keith A.,Wells, Gregory J.
, p. 259 - 262 (2007/10/02)
Reaction of lithio 1-trimethylsilylcyclopropane or its formal equivalent with carbonyl compounds leads to carbinols which dehydrate without rearrangement.Other attempts to induce ring expansion of the silicon substituted three-membered ring by i
