7 research outputs found
Aplicação de α-oxoceteno ditiocetais em sĂntese orgĂąnica Reactivity of α-oxoketene dithiocetals in organic synthesis
<abstract language="eng">The synthesis and reactivity of α-oxoketenes dithioacetals (S,S-acetals), general structure [(RÂčC=OC(RÂČ)=C(SRÂł)(SR4)], are reported. We also showed the application of S,S acetals as synthons for efficient synthesis of isoxazoles, pyrazoles, indazoles, thiophenes, dithiol thiones, pyridines, pyrimidines and other heterocycles. This work aims to review the importance of α-oxoketenes dithioacetals in organic chemistry during the past few years
7-Chloroquinolin-4-yl Arylhydrazone Derivatives: Synthesis and Antifungal Activity
Fifteen 7-chloro-4-arylhydrazonequinolines have been evaluated for their in vitro antifungal activity against eight oral fungi: Candida albicans, C. parapsilosis, C. lipolytica, C. tropicalis, C. famata, C. glabrata, Rhodutorula mucilaginosa, and R. glutinis. Several compounds exhibited minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) activities comparable with the first-line drug fluconazole. These results could be considered as an important starting point for the rational design of new antifungal agents
Synthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitors
A series of nineteen benzothiazin-4-ones from N-(3-aminopropyl) piperidine, 4-(2-aminoethyl)morpholine or 1-(2-aminoethyl)piperidine, aliphatic or aromatic aldehyde and thiosalicylic acid, were synthesized in good yields by multicomponent one-pot reactions. The solvent was toluene and this efficient procedure afforded the desired heterocycles in 5âh. Identification and characterization were achieved by NMR and GCâMS techniques. In vitro AChE activities of all compounds were evaluated in cerebral cortex and hippocampus of rats and in general, the results in cortex were more promising than hippocampus. The benzothiazinone 5Bd showed the best AChE inhibition activity IC50 8.48âÎŒM (cortex) and IC50 39.80âÎŒM (hippocampus). The cytotoxicity of seven compounds in MCR-5 human fibroblast cell by SRB test in 24âh were evaluated and 5Bd suggest preliminary safety, showing no cytotoxicity at 100 ”M. Finally, these important findings could be a starting point for the development of new AChE inhibitors agents and will provide the basis for new studies