SYNTHESIS OF 4-METHYL-SUBSTITUTED CIS-5-ARYLPROLINES – POTENT INHIBITORS OF STAPHYLOCOCCUS AUREUS SORTASE A AND THROMBIN (FACTOR IIa) |
| 3 | |
| 2013 |
| scientific article | 547.747; 543.429.23; 539.26 | ||
| 94-101 | vinyl sulfone, azomethine ylide, 1,3-dipolar cycloaddition, correlation NMR spectroscopy, X-ray analysis. |
| A 1,3-dipolar cycloaddition between methyl (vinyl)-, ? -bromvinyl (methyl)- and benzyl (vinyl) sulfones and azomethines (generated from N -arylimines of methyl and ethyl esters of glycine and alanine) takes place in toluene at 20?C under the influence of catalytic additives of silver acetate and triethylamine resulting in production of sulfonyl-substituted cis -5-arylprolines. The latter exhibit a wide range of biological activity and can be considered as a basis for drugs with selective action. The structure of cis -5-arylprolines is discussed. |
 |