N,N'-disubstituted urea-based soluble epoxide hydrolase (sEH) inhibitors are promising therapeutics for hypertension, inflammation, and pain in multiple animal models. The drug absorption and pharmacological efficacy of these inhibitors have been reported extensively. However, the drug metabolism of these inhibitors is not well described. Here we reported the metabolic profile and associated bi...

The X-ray crystal structure of arginase from Schistosoma mansoni (SmARG) and the structures of its complexes with several amino acid inhibitors have been determined at atomic resolution. SmARG is a binuclear manganese metalloenzyme that catalyzes the hydrolysis of l-arginine to form l-ornithine and urea, and this enzyme is upregulated in all forms of the parasite that interact with the human ho...

Divergent syntheses of indolizines and 2,4-disubstituted pyrroles by the silver-catalyzed cyclization of 2-pyridyl alkynyl carbinols with isocyanides are reported. These methods provide an effective route to highly functionalized indolizines and 2,4-disubstituted pyrroles in good to excellent yields. The 2,4-disubstituted pyrroles are synthesized by an unprecedented regioselective [3+2] cycload...

The title compound, C23H21N3O2, is constructed about an almost planar disubstituted amino-urea residue (r.m.s. deviation = 0.0201 Å), which features an intra-molecular amine-N-H⋯N(imine) hydrogen bond. In the 'all-trans' chain connecting this to the terminal meth-oxy-benzene residue, the conformation about each of the imine and ethyl-ene double bonds is E. In the crystal, amide-N-H⋯O(carbon-yl)...

A series of N,N'-disubstituted ureas having a conformationally restricted cis- or trans-1,4-cyclohexane alpha to the urea were prepared and tested as soluble epoxide hydrolase (sEH) inhibitors. This series of compounds showed low nanomolar to picomolar activities against recombinant human sEH. Both isomers showed similar potencies, but the trans isomers were more metabolically stable in human h...

The dominant alkaloids previously identified in skin extracts of Amazonian dendrobatid frogs of the genus Ameerega are histrionicotoxins and 2,5-disubstituted decahydroquinolines. Analysis of alkaloids in skin extracts of Ameerega picta from Bolivia revealed that the alkaloid 257A, previously reported as a 2,5-disubstituted decahydroquinoline, is an N-methyl-2,5-disubstituted decahydroquinoline...

A simple color change detection by the naked-eye using paper-strip for a biologically relevant fluorine (F–) anion in water is challenge. New non-planar push–pull chromophore involving intramolecular charge-transfer (ICT) from urea donor 2,3-disubstituted-1,1,4,4-tetracyanobuta-1,3-diene (TCBD) turns out to be an efficient system detecting F– ion giving various output signals. But, replacing ph...