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A novel class of substituted benzo[d]imidazo[5,1-b]thiazol-1-amine derivatives was synthesized utilizing a one-pot Cu-catalyzed cycloaddition of benzothiazole, trichloroacetonitrile, various amines and terminal alkynes in acetonitrile at room temperature. The speed of this simple four-component reaction along with mild conditions, high yields, readily available starting materials, the ease of work-up without using pollutant precious metals–catalysts, and column chromatography are important features of the presented procedure. [ABSTRACT FROM AUTHOR]

An efficient synthesis of highly substituted thiophenes was developed by means of sulfonylketenimines in a multi-step reaction including heterocumulene system containing sulfur and nitro-alkanes with acidic α-hydrogen. The speed and ease of conducting this four-component reaction under mild conditions and using available materials makes it an ideal method to synthesize high purity substituted thiophenes with sulfonamide moiety. All structures synthesized are confirmed by the instrumental analysis (EI-MS, IR and 1H /13C-NMR). [ABSTRACT FROM AUTHOR]

Introduction: The attractive biological actions of the eicosatrienoic acids (EETs) and endocannabinoids (eCBs) are terminated by means of enzymatic hydrolysis via soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FAAH) enzymes. Simultaneous inhibition of both enzymes is considered a novel approach in the treatment of inflammatory and neuropathic pain., Methods: In this study, a novel series of tetrazole derivatives as dual sEH/FAAH inhibitors were designed, synthesized, and biologically evaluated. Compounds 6c, 7d, and 8a, the most potent inhibitors against FAAH and sEH enzymes with acceptable IC 50 values, significantly decreased carrageenan- induced paw edema 5h after carrageenan injection compared to the control group compound. In addition, compound 7d exhibited a significant reduction in pain scores compared to the control group., Results: Docking studies showed that the presented dual inhibitors could bind to the essential residues in the catalytic sites of both enzymes. In silico prediction of several pharmacokinetic properties suggests that these dual inhibitors could potentially be orally active agents., Conclusion: These structures will be a valuable scaffold to develop soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)