Multifunctional Isosteric Pyridine Analogs-Based 2-Aminothiazole: Design, Synthesis, and Potential Phosphodiesterase-5 Inhibitory Activity

Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds

A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as antitrypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four of eleven compounds were moderately active against Leish...

Synthesis and protein tyrosine phosphatase inhibitory activity of dephostatin analogs.

We have synthesized derivatives of dephostatin, a protein tyrosine phosphatase (PTPase) inhibitor, to study the structure-activity relationships of this inhibitor. Inactive analogs revealed some insight into structural requirements or PTPase inhibitory activity of dephostatin. Both a nitroso group and phenolic hydroxyl groups were found to be essential for the inhibitory activity. Among the dep...

Synthesis and antifungal activity of benzimidazole, benzotriazole and aminothiazole derivatives

In recent years, the use of antifungal drugs in human medicine has increased, especially with the advent of AIDS epidemic. Efforts have focused on the development of new, less toxic and more efficacious antifungal drugs with novel mechanism of action. The purpose of this study was to synthesize of some new benzimidazole, benzotriazole and aminothiazole derivatives and to evaluate their activity...

design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues

Synthesis of New Pyridine Based 4-Thiazolidinones Incorporated Benzothiazoles and Evaluation of Their Antimicrobial Activity

Substituted Schiff bases (hydrazones) 5a-j have been prepared from the starting material 2-chloro pyridine-3-carboxylic acid 1 by a sequence of reactions like reaction with 2-amino-6-nitro benzothiazole (Ullamann condensation), thionyl chloride, hydrazine hydrate and different aromatic aldehydes. On cyclocondensation of 5a-j with thioglycolic acid in dry 1,4-dioxane furnished desired compounds ...