Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine

Synthesis and anticancer activity of some thiophene, thienyl‐thiazole, and thienyl‐benzofuran analogues

“…to generate the 2-(thienylimino)thiazolidin-4-one intermediate 17. The unexpected ring closure of the intermediate 17 through nucleophilic addition of the imino group (=NH-) on the nitrile group resulted in the formation of thiazolo[3,2-a]thiazolo[2,3-d]pyrimidine ring system 18.Many different configurations of the fused rings thiazolo[3,2-a]thieno[2,3-d]pyrimidine allow for a wide range of applications in fields such as technology, medicine, and agriculture[35,36]. Spectroscopic methods were used to confirm the structure of the thiazolo[3,2-a] thieno[2,3-d]pyrimidine derivative 18.…”

Three-Step Synthetic Pathway toward Fully Decorated [1,2,3]Triazolo[4,5-d]pyrimidine (8-Azapurine) Derivatives

“…The [1,2,3]­triazolo­[4,5- d ]­pyrimidine (8-azapurine) (Figure ) scaffold is known to be a bioisostere of the purine nucleus, and derivatives have been widely studied for their medicinal properties (e.g., 8-azaadenosine, zaprinast; Figure ). − A marketed example is ticagrelor (Brilinta), which acts as a platelet aggregation inhibitor in patients with acute coronary syndrome (Figure ). Furthermore, many 8-azapurines have shown intrinsic fluorescence properties which were used to monitor reactions and their kinetics, interaction modes with enzymes, and metabolic pathways involving purines and analogues. − The utility of 8-azapurines was already demonstrated in multiple domains, making them interesting scaffolds for further evaluation.…”