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The incorporation of brominated flame retardants into industrial and household appliances has increased their occurrence in the environment, resulting in deleterious effects on wildlife. With the increasing restraints on available compounds, there has been a shift to using brominated flame
This application discloses a series of di- and tri-substituted cyclohexanes as CCR2 receptor antagonists which are stated to be useful in treating inflammation and autoimmune diseases, such as type 2 diabetes and asthma. Although receptor binding of the compounds to CCR2 is demonstrated, there are
We have discovered a novel series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists. Divergent SAR studies on hCCR2 and hERG activities led to the discovery of compound 8d, which displayed good hCCR2 binding affinity (IC50, 37 nM) and potent functional antagonism (chemotaxis IC50, 30 nM). It
A novel series of leukotriene B4 (LTB4) antagonists is reported. These compounds present a cyclohexane ring in their chemical structure, which mimics the three conjugated double bonds of LTB4. The biochemical/pharmacological profile of the leader compound, PH-163 (sodium
Both Gram-positive and Gram-negative pathogens or pathogen-derived components, such as staphylococcal enterotoxins (SEs) and endotoxin (LPS) exposure, activate MyD88-mediated pro-inflammatory cellular immunity for host defense. However, dysregulated MyD88-mediated signaling triggers exaggerated
Although a promising strategy, the mesenchymal stem cell (MSC)-based therapy of cartilage defects is sometimes accompanied with chronic inflammation during the remodeling status, which may hinder cartilage regeneration. During this process, the inflammatory cytokine tumor necrosis factor α (TNFα)
The octocoral-derived terpenes fuscol and eunicol are known, potent anti-inflammatory agents. While total syntheses of one of the parent natural products have been published, the economic and practical feasibility of producing commercially viable amounts of material is very low. Based on the
The singlet excited-state quenching of Acridine Orange (AO) by methyl viologen (MV2+) and the non-steroidal anti-inflammatory drug Piroxicam (Prx), incorporated in sodium bis(2-ethylhexyl) sulfosuccinate (AOT)/isooctane/water and Triton X-100 (Trx-100)/cyclohexane-hexanol/water (w/o) microemulsions,
This study was conducted to examine the tyrosinase inhibitory and anti-inflammatory activities of kojic acid derivatives. A series of kojic acid derivatives containing thioether, sulfoxide, and sulfone linkages were synthesized. In the tyrosinase assay, kojyl thioether derivatives containing
Alternate forms of drug crystals display different physicochemical properties. These include stability, dissolution rate, bioavailability and solubility, which can affect pharmacokinetics and pharmacodynamics. It is therefore important to compare the crystal forms of cedrol to obtain optimal
OBJECTIVE
A series of tetraketones has been synthesized by way of a one pot synthesis and screened for inhibitory activity against the enzyme lipoxygenase.
METHODS
An efficient and high yielding one pot synthesis to tetraketones [2-22] has been developed by way of tetraethyl ammonium bromide
A series of 1-hydroxy-3-¿3-hydroxy-7-phenyl-1-hepten-1-yl cyclohexane acetic acid derivatives was designed based on postulated active conformation of leukotriene B(4) (LTB(4)) and evaluated as human cell surface LTB(4) receptor (BLTR) antagonists. Binding was determined through ¿(3)HLTB(4)
In this study, the severity and time course of inflammation induced by 4 organic solvents (acetone, cyclohexane, toluene and m-xylene), and the effect of neuropeptides during the inflammation were investigated in the hairless rat abdominal skin. Plasma extravasation used as a parameter of
Infection triggers the release of pro-inflammatory cytokines (TNF-alpha and IL-6). Over-production, however, cause tissue injury seen in severe asthma. The ability of enaminone E121 to reduce pro-inflammatory cytokines in our laboratory encouraged further examination of its structural scaffold.