Pateamine A is a naturally occurring metabolite extracted from the marine sponge Mycale hentscheli. It exhibits potent cytotoxicity towards cancer cell lines and has been shown to target protein translation initiation via inhibition of the function of eukaryotic initiation factor 4A proteins. We have synthesised a simplified analogue of pateamine A, consisting of the skeletal core of the natura...

Quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. Thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. Due to valuable cytotoxic effects of both thiazole gr...

The current study examined the bioactivation potential of ghrelin receptor inverse agonists, 1-{2-[2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]2,7-diazaspiro[3.5]nonan-7-yl}-2-(imidazo[2,1-b]thiazol-6yl)ethanone (1) and 1-{2-[2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7diazaspiro[3.5]nonan-7-yl}-2-(2-methylimidazo[2,1-b]thiazol-6-yl) ethanone (2), containing a fused imidazo[2,1-b]thiazole motif i...

quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. due to valuable cytotoxic effects of both thiazole gr...

The solid-solid reactions of thiosemicarbazide with 4-formylantipyrine, 2-acetylpyrrole and camphor were performed to afford the thiosemicarbazones 1-3 which underwent hetero-cyclization with phenacyl bromide to furnish the corresponding thiazole derivatives 4-6. The yields of the reactions are quantitative in all cases and the products do not require further purification. A series of 5-arylazo...

The current study examined the bioactivation potential of ghrelin receptor inverse agonists, 1-{2-[2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]nonan-7-yl}-2-(imidazo[2,1-b]thiazol-6-yl)ethanone (1) and 1-{2-[2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]nonan-7-yl}-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone (2), containing a fused imidazo[2,1-b]thiazole motif...

starting from readily available 2-substituted-4-methylthiazole-5-carboxylic acid hydrazide (1), the title compounds were prepared. the reaction of compound 1 (r=ch3) with formic acid yielded 1-(formyl)-2-(2,4-dimethylthiazole-5-carboxyl) hydrazine (2). refluxing the latter with phosphorous pentasulfide in xylene afforded compound 3, the reaction of compound 2 with phosphorous pentoxide afforded...

In this study, we report a novel hydrate former that acts as structure II (sII) and thermodynamic inhibitor. Thiazole is an aromatic five-ringed molecule with two heteroatoms. forms sII crystal small CH4 CO2 molecules. The Rietveld refinement result of (CH4 + thiazole) positions the thiazole off center 51264 cages, S N atoms face O at apex pentagonal faces one hexagonal cage, respectively. Cons...

A series of multidentate N-donor ligands have been synthesised all containing pyridyl and pyridyl/thiazole units and their coordination behaviour is described. The ligands are classified into four types; i) terpyridine containing pyridyl/thiazole ligands (L); ii) pyridyl/thiazole ligands containing a 3,3′-disubstituted bipyridine core. (L); iii) 2,2′-bipyridine containing a crown ether moiety (...