To find a reasonable way to prepare the designed CPP32 inhibitors. Method Ugifour-component condensation reaction was used to synthesize peptide mimic CPP32 inhibitors; ResultsA key isocyanide component (aspartate-derived isocyanide 3) and one of the designed CPP32inhibitors 4 (as a template) were synthesized; Conclusion The CPP32 inhibitor 4 was synthesized bythe newly developed procedure, which is an Ugi four-component condensation reaction based onaspartate-derived isocyanide 3. This method can be used to build up the CPP32 inhibitor library.
To study the antifungal effect of chalcone derivatives. Methods Sixteenchalcone derivatives were synthesized and confirmed by ~1H NMR and IR spectra, and tested forantifungal activity against four common pathogenic fungi. Their structure-activity relationship isdiscussed. Results Among 16 title compounds, there were 5 new compounds, which have not beenreported before. The preliminary antifungal test showed that all title compounds exhibitedantifungal activities to a certain extent. The activity of compound 8 against Trichophyton rubrumhad a potency equal to that of fluconazole, with a MIC of 4 μg·mL^(-1) . Conclusion Sixteenchalcones were prepared and their antifungal activities against four common pathogenic fungi invitro were examined. Some of them exhibited antifungal activities to a certain extent.
The total synthesis of a hydrated aurone derivative, 2-benzyl-4-methoxy-2,6-dihydroxybenzofuran-3（2H）-one, has been achieved for the first time with 2.4% overall yield. Using phloroglucinol as the starting material, the key steps included Friedel-Crafts acylation, Williamson synthesis, hydrogenolysis, aldol condensation, enolization and Rubottom oxidation.
CGRP receptor（CLR） is a B class GPCR that functions only when combined with RAMPs. CLR/RAMP1 has been regarded as a promising target for migraine treatment, as its antagonists have been proved to be effective recently. In the present study we designed and synthesized small molecular antagonists against CLR/RAMP1, resulting in a novel type of structure with acceptable high potency. The molecules were designed via virtual screening. Afterwards, a series of modification were conducted on the hit compounds, resulting in compound 8 as the best scored compound in docking, which was further validated in vitro by cell-based functional assay.
