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EnglishA convenient approach to the synthesis of alkyl esters of aspirin (ASA-OR) has been developed. The synthesis of ASA-OR has been realized in two steps: (1) direct esterification of salicylic acid with alcohols in the presence of dicyclohexylcarbodiimide to give alkyl salicylates (SAL-OR); (2) acetylation of SAL-OR with acetyl chloride to yield ASA-OR. Molecular mechanics simulations, performed to calculate the kinetic radii of several ASA-OR, indicated that the pentyl and hexyl acetylsalicylates possess the best properties to cross cell membranes. The in vitro biological tests demonstrate their anti-inflammatory activity, superimposable to that of aspirin. The results of our study suggest that ASA-OR may be used as anti-inflammatory drugs for topical application.
Mancuso, R., Ferlazzo, N., De Luca, G., Amuso, R., Piccionello, A., Giofrè, S., et al. (2019). Synthesis, computational evaluation and pharmacological assessment of acetylsalicylic esters as anti-inflammatory agents. MEDICINAL CHEMISTRY RESEARCH, 28(3), 292-299 [10.1007/s00044-018-02284-3].
| Data di pubblicazione: | 2019 | |
| Titolo: | Synthesis, computational evaluation and pharmacological assessment of acetylsalicylic esters as anti-inflammatory agents | |
| Autori: | ||
| Citazione: | Mancuso, R., Ferlazzo, N., De Luca, G., Amuso, R., Piccionello, A., Giofrè, S., et al. (2019). Synthesis, computational evaluation and pharmacological assessment of acetylsalicylic esters as anti-inflammatory agents. MEDICINAL CHEMISTRY RESEARCH, 28(3), 292-299 [10.1007/s00044-018-02284-3]. | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1007/s00044-018-02284-3 | |
| Abstract: | A convenient approach to the synthesis of alkyl esters of aspirin (ASA-OR) has been developed. The synthesis of ASA-OR has been realized in two steps: (1) direct esterification of salicylic acid with alcohols in the presence of dicyclohexylcarbodiimide to give alkyl salicylates (SAL-OR); (2) acetylation of SAL-OR with acetyl chloride to yield ASA-OR. Molecular mechanics simulations, performed to calculate the kinetic radii of several ASA-OR, indicated that the pentyl and hexyl acetylsalicylates possess the best properties to cross cell membranes. The in vitro biological tests demonstrate their anti-inflammatory activity, superimposable to that of aspirin. The results of our study suggest that ASA-OR may be used as anti-inflammatory drugs for topical application. | |
| URL: | http://www.springerlink.com/content/1054-2523 | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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http://hdl.handle.net/10447/351104
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