328557-06-8Relevant articles and documents
Solvothermal synthesis of multiple dihydropyrimidinones at a time as inhibitors of Eg5
Chen, Dan,Chen, Shi-Quan,Jiang, Xiao-Qiang,Liu, Yan-Fei,Pan, Xin-Guang,Wang, Shi-Fan
, (2021)
Solvothermal synthesis of multiple dihydropyrimidinones at a time has been developed in inexpensive and green bio-based solvent lactic acid without any additional catalysts or additives. By this method, thirty new dihydropyrimidinone derivatives were synthesized in two batches and characterized. All of the compounds were screened by Eg5 motor protein ATPase assay, and the positive compounds were tested against the Caco-2 cell line, HeLa cell line, L929 cell line and T24 cell line in vitro. Among them, compound C9 exhibited the best inhibitory activity against motor protein ATPase with an IC50 value of 30.25 μM and significant cytotoxic activity in the micromolar range against the cells above. The Lineweaver–Burk plot revealed that compound C9 was a mixed-type Eg5 inhibitor. A molecular modeling study using the Discovery Studio program was performed, where compound C9 exhibited good binding interaction with Eg5 motor protein ATPase, and this was consistent with the attained experimental results.
Catalyst-free, rapid synthesis of fused bicyclic thiazolo-pyrimidine and pyrimido-thiazine derivatives by a microwave-assisted method
Virsodia, Vijay R.,Vekariya, Nikhil R.,Manvar, Atul T.,Khunt, Rupesh C.,Marvania, Bhavin R.,Savalia, Bharat S.,Shah, Anamik K.
body text, p. 34 - 44 (2009/04/16)
The present investigation deals with the rapid microwave-assisted synthesis of compounds containing fused bicyclic systems. Dihydropyrimidines obtained via a microwave-assisted Biginelli reaction were treated with dibromo alkanes under microwave condition
Synthesis of some new 1,2,3,4-tetrahydropyrimidine-2-thiones and their thiazolo[3,2-α]pyrimidine derivatives as potential biological agents
Akbari,Kachhadia,Tala,Bapodra,Dhaduk,Joshi,Mehta,Pathak
experimental part, p. 1911 - 1922 (2009/06/30)
Some new N-(4-chlorophenyl)-6-methyl-4-aryl-2-thioxo-1,2,3,4-tetrahydro pyrimidine-5-carboxamide 4(a-h) were synthesized by the reaction of N-(4-chlorophenyl)-3-oxobutanamide, thiourea and different aromatic aldehydes. The synthesis of N-(4-chlorophenyl)-7-methyl-5-aryl-2,3-dihydro-5H-thiazolol[3, 2-a]pyrimidine-6-carboxamide 5(a-h) was accomplished by cyclocondensation of 1,2,3,4-tetrahydropyrimidine-2-thiones 4(a-h) and 1,2-dibromoethane. The structures of these compounds have been proved by IR, 1H-NMR, and Mass spectral studies. Synthesized compounds 4(a-h) and 5(a-h) were evaluated for their antimicrobial activities. Some of the compounds exhibited significant inhibition on bacterial and fungal growth as compared to standard drugs. Copyright Taylor & Francis Group, LLC.