Synthesis and Biological Evaluation of Novel Thiazolyl-Coumarin Derivatives as Potent Histone Deacetylase Inhibitors with Antifibrotic Activity.

New histone deacetylases (HDAC) inhibitors with low toxicity to non-cancerous cells, are a prevalent issue at present because these enzymes are actively involved in fibrotic diseases. We designed and synthesized a novel series of thiazolyl-coumarins, substituted at position 6 (R = H, Br, OCH₃), linked to classic zinc binding groups, such as hydroxamic and carboxylic acid moieties and alternative zinc binding groups such as disulfide and catechol. Their in vitro inhibitory activities against HDACs were evaluated.

Chromenopyridines: promising scaffolds for medicinal and biological chemistry.

Chromenopyridines constitute a structurally diverse class of compounds with a wide range of bioactivities and increasing presence in drugs. Here we analyze the scope of the synthetic methodology to access this nucleus with emphasis on multicomponent reactions and robust methodologies. Reactivity issues, medicinal applications and other properties are also reviewed.

Oxidation of C4-hydroxyphenyl 1,4-dihydropyridines in dimethylsulfoxide and its reactivity towards alkylperoxyl radicals in aqueous medium.

This work reports the electrochemical oxidation of three newly synthesized C4-hydroxyphenyl-substituted 1,4-dihydropyridine derivatives in dimethylsulfoxide. The reactivity of the compounds with ABAP-derived alkylperoxyl radicals in aqueous buffer pH 7.4, was also studied.

Analyses by GC-MS and GC-MS-MS of the Hantzsch synthesis products using hydroxy- and methoxy-aromatic aldehydes.

EI mass spectra of products of the dihydropyridine Hantzsch synthesis using hydroxy and methoxy aldehydes as starting materials are reported. The reaction products (C-4 hydroxy- and methoxyphenyl-1,4-dihydropyridines and chromeno[3,4,c]-pyridines) were derivatized with N-methyl-N-(trimethylsilyl)-trifluoracetamide to be analyzed by gas chromatographic techniques. Fragmentation pathways for 1,4-dihydropyridines and chromeno-pyridines are proposed.

Electrochemical and EPR characterization of 1,4-dihydropyridines. Reactivity towards alkyl radicals.

This work reports the electrochemical oxidation of a series of three synthesized 4-substituted-1,4-dihydropyridine derivatives in different electrolytic media. Also, an EPR characterization of intermediates and the reactivity of derivatives towards ABAP-derived alkyl radicals are reported. Dynamic, differential pulse and cyclic voltammetry studies on a glassy carbon electrode showed an irreversible single-peak due to the oxidation of the 1,4-dihydropyridine (1,4-DHP) ring via 2-electrons to the corresponding pyridine derivative.