Synthesis and AChE inhibiting activity of 2, 4 substituted 6-Phenyl Pyrimidines
- Novel substituted pyrimidines were synthesized from methyl 2,4-dioxo-4-phenyl-butanoate (I-A) and urea, followed by Mitsunobu coupling of I-A with benzyl or allyl alcohol to give the corresponding 2-hydroxypyrimidine ethers in good yields. Saponification of I-A, followed by reaction with benzyl or allyl amines in the presence of TBTU yielded 2-hydroxy-6-phenyl-pyrimidine 4-carboxamides. AChE and BuChE assays revealed 2-hydroxy-6-phenyl-pyrimidine-4-carboxyallyamide as the most active compound, IC50=90 mu M, with no inhibition of BuChE.
| Author details: | Cristian PazORCiD, Martin G. Peter, Bernd SchmidtORCiDGND, Jose Becerra, Margarita Gutierrez, Luis Astudillo, Mario Silva |
|---|---|
| ISSN: | 0717-9324 |
| Title of parent work (English): | Journal of the Chilean Chemical Society |
| Publisher: | Sociedad Chilena De Quimica |
| Place of publishing: | Concepcion |
| Publication type: | Article |
| Language: | English |
| Year of first publication: | 2012 |
| Publication year: | 2012 |
| Release date: | 2017/03/26 |
| Tag: | Pyrimidines; TBTU; inhibition AChE; mitsunobu |
| Volume: | 57 |
| Issue: | 3 |
| Number of pages: | 3 |
| First page: | 1292 |
| Last Page: | 1294 |
| Funding institution: | Universidad de Concepcion; CONICYT |
| Organizational units: | Mathematisch-Naturwissenschaftliche Fakultät / Institut für Chemie |
| Peer review: | Referiert |
| Publishing method: | Open Access |
