Chen, Ying published the artcileStructure-activity relationship studies of (E)-3,4-dihydroxystyryl alkyl sulfones as novel neuroprotective agents based on improved antioxidant, anti-inflammatory activities and BBB permeability, Name: (2-Bromoethyl)cyclopentane, the publication is European Journal of Medicinal Chemistry (2019), 420-433, database is CAplus and MEDLINE.
(E)-3,4-dihydroxystyryl alkyl sulfones I [n = 0, 1, 2; R = Et, Pr, Bu, etc.], as new analogs of neurodegenerative agents, were designed and synthesized. The biol. 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, I [n = 2; R = cyclopentyl] exhibited prominent antioxidant activity at low concentration (2.5 μM) in H2O2 model (cell viability = 94.5%). In addition, I [n = 2; R = cyclopentyl] (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 I [n = 2; R = cyclopentyl], the apoptotic rates of H2O2-damaged PC12 cells were detected by Annexin V-FITC/PI assay. I [n = 2; R = cyclopentyl] 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 x 10-6 cm s-1), low cytotoxicity and favorable physiochem. properties based on calculation, compound I [n = 2; R = cyclopentyl] can be further developed as a potential multifunctional neuroprotective agent.
European Journal of Medicinal Chemistry published new progress about 18928-94-4. 18928-94-4 belongs to bromides-buliding-blocks, auxiliary class Bromide,Aliphatic cyclic hydrocarbon, name is (2-Bromoethyl)cyclopentane, and the molecular formula is C7H13Br, Name: (2-Bromoethyl)cyclopentane.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary