2550-36-9Relevant articles and documents
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.
SYNTHESIS METHOD FOR L-CYCLIC ALKYL AMINO ACID AND PHARMACEUTICAL COMPOSITION HAVING THEREOF
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Paragraph 0083, (2016/11/17)
A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD+, and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is where n1≧1, m1≧0 and the M1 is H or a monovalent cation; the Structural Formula (II) is where n2≧0, m2≧0, the M2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.
Photochemistry of Alkyl Halides. 9. Geminal Dihalides
Kropp, Paul J.,Pienta, Norbert J.
, p. 2084 - 2090 (2007/10/02)
The photobehavior of the geminal dihalides (diiodomethyl)cyclohexane (7), (bromoiodomethyl)cyclohexane (11), (dibromomethyl)cyclohexane (17), (diiodomethyl)cyclopentane (22), 3,3-dimethyl(diiodomethyl)cyclobutane (27), and 8,8-diiodo-2,6-dimethyl-2-octene (31) has been studied and compared with that previously observed for diiodomethane.In all solvents the corresponding vinyl halides (iodomethylene)cyclohexane (13), (bromomethylene)cyclohexane (21), (iodomethylene)cyclopentane (23), 3,3-dimethyl(iodomethylene)cyclobutane (28), or cis- and trans-3,7-dimethyl-1-iodo-1,6-octadiene (33) were obtained, which are thought to arise from α-halo cationic intermediate formed via initial light-induced homolytic cleavage of the carbon-iodine bond followed by electron transfer within the resulting caged radical pair, as shown in Schemes II and III.In the case of diiodide 31 competing intramolecular trapping of the α-iodo cation afforded in addition the cyclized isopulegyl iodide (34).In polar solvents the vinyl iodides were accompanied by the nonhalogenated products methylenecyclohexane (15), 1-methylcyclopentene (25), cyclohexene (26), 4,4-dimethylcyclopentene (29), and cis- and trans-carane (35), which are thought also to arise from the α-halo cationic intermediate. 1.1-Diiodo-2,2-dimethylpropane (1b) afforded 2-methyl-2-butene (6b).Except for carane (35) from diiodide 31 there was no detectable formation of cyclopropanes.In methanol the nucleophilic substitution products (dimethoxymethyl)cyclohexane (14), (dimethoxymethyl)cyclopentane (24), and 1,1-dimethoxy-2,2-dimethylpropane (30) were obtained.It is concluded that geminal dihalides undergo predominant, if not exclusive, photoreaction via initial clea vage of a single carbon-halogen bond in analogy with monohalides and that carbene intermediates are not formed.A similiar conclusion has been reached previously for diiodomethane in the photocyclopropanation of alkenes.