Based on the extensive biological activities of thiazole derivatives against different types of diseases, we are interested in the effective part of many natural compounds, so we synthesized a new series of compounds containing di-, tri- and tetrathiazole moieties. The formation of such derivatives proceeded via reaction of 2-bromo-1-(4-methyl-2-(methylamino)thiazol-5-yl)ethan-1-one with heterocyclic amines, o-aminothiophenol and thiosemicarbazone derivatives. The structure and mechanistic pathways for all products were discussed and proved based on spectral results, in addition to conformational studies. Our aim after the synthesis is to investigate their antimicrobial activity against various types of bacteria and fungi species. Preceeding such an investigation, a molecular docking study was carried out with selected conformers, as representative examples, against three pathogen-proteins. This preliminary stage could support the biological application. The potency of these compounds as antimicrobial agents has been evaluated. The results showed that derivatives which have di- and trithiazole rings displayed high activity that exceeds the used standard antibiotic.

https://www.mdpi.com/1420-3049/24/9/1741/pdf

New Series of Thiazole Derivatives: Synthesis, Structural Elucidation, Antimicrobial Activity, Molecular Modeling and MOE Docking.

Discovery of thiazole-based-chalcones and 4-hetarylthiazoles as potent anticancer agents: Synthesis, docking study and anticancer activity.

Current scenario of indole derivatives with potential anti-drug-resistant cancer activity.

The isatin framework is a useful template for the development of novel anticancer agents. This is exemplified by the fact that several isatin-based anticancer agents, such as semaxanib, sunitinib, nintedanib, and hesperadin, are already in use or under clinical trials for the treatment of diverse kinds of cancers. Isatin-based hybrids could be obtained by incorporating other anticancer pharmacophores into the isatin skeleton and they have the potential to overcome drug resistance with reduced side effects. Thus, isatin-based hybrids may provide attractive scaffolds for the development of novel anticancer agents. This review covers the recent advances of isatin-based hybrids with anticancer activity, covering articles published between 2001 and 2019. The anticancer activities of these molecules and the structure-activity relationships are also discussed. The purpose of this review article is to set up the direction for the design and development of isatin-based hybrids with high efficacy and low toxicity.

Recent advances in isatin hybrids as potential anticancer agents

Investigation on corrosion protection behavior and adsorption of carbohydrazide-pyrazole compounds on mild steel in 15% HCl solution: Electrochemical and computational approach

New series of 1,3,4-thiadiazoles have been prepared via reaction of 1,3,4-thiadiazolenaminones 1 with N-phenyl 2-oxopropanehydrazonoyl chloride (2) in dioxane in the presence of triethylamine. Also, some new heterocycles incorporating 1,3,4-thiadiazole ring were obtained by reaction of 1,3,4-thiadiazolenaminones 1 with nitrogen-nucleophiles like hydrazine hydrate, 3-amino-1,2,4-triazole and 2-aminobenzimidazole. The structure of the new products was established based on elemental and spectral analysis. The relation between the structure of the products and their activity towards some microorganisms was studied and promising results were obtained.

Mohamed R. Abdel Aziz

Papers

Synthesis and antimicrobial activity of some new 1,3,4-thiadiazole derivatives.

Novel Nano‐sized bis‐indoline Derivatives as Antitumor Agents

Synthesis of a Novel Tri‐enaminone as Building Block for Polyaza‐heterocycles