Some examples of the diverse research done by chemistry experts include discovery of new medicines and vaccines, improving understanding of environmental issues, and development of new chemical products and materials. In a pantent, Dipyrimido[4,5-b:5,4-e][1,4]thiazine: synthesis and their enzyme inhibitory activity assessment on soybean 15-lipoxygenase. Application In Synthesis of Campathecin.
Dipyrimido[4,5-b:5,4-e][1,4]thiazine: synthesis and their enzyme inhibitory activity assessment on soybean 15-lipoxygenase
A series of new derivatives of dipyrimido[4,5-b:5,4-e][1,4] thiazine were synthesized by treatment of 5-amino-6-methyl-2-morpholino-4-pyrimidinethiol (1) with 5-bromo-2,4-dichloro-6-methylpyrimidine (2) in the presence of triethylamine and ethanol and subsequently with various secondary amines in EtOH/DMF. The thioether derivative 3 and heterocyclization products 4a-f were characterized by elemental analysis and spectroscopic techniques. The 15-LO inhibitory activities of the new synthesized compounds were also evaluated. The results show that compound 4e has the best IC50 of 15-LO inhibition (IC50 = 14.4 A mu M) but when all the products were theoretically docked into 15-LO, the GOLD scores of compounds 4e and 4d are 43.67 and 43.39 respectively, which show the best results. We suggest that the hydrogen bond interaction between Ser489 of 15-LO and the nitrogen of piperazine ring of compound 4e appears to play major role in lipoxygenase inhibition.
I am very proud of our efforts over the past few months and hope to 7689-03-4 help many people in the next few years. Application In Synthesis of Campathecin.
Reference:
Thiazine – an overview | ScienceDirect Topics,
,Thiazine | C4H5NS – PubChem