Aspirin prodrugs: synthesis of 2-substituted 2-methyl-4H-1,3-benzodioxin-4-ones and their screening for prodrug potential.
A series of new 2-substituted 2-methyl-4H-1,3-benzodioxin-4-ones 1 have been synthesized and fully characterized. This study involves fifteen compounds of which fourteen are orthoesters, containing tertiary aliphatic alkoxy groups. One compound contains a tert-butylperoxy group and one a 3 beta-cholesteryloxy group in the 2-position. The hydrolysis of these compounds 1 was followed in enzymatic and non-enzymatic media to clarify whether they are true prodrugs of aspirin. Two compounds 1 were additionally tested in vivo as potential topical keratolytics.
Nielsen,Senning
p. 952 - 956
(2007/10/02)
Chemical feasibility studies concerning potential prodrugs of acetylsalicylic acid
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Hansen,Senning
p. 351 - 359
(2007/10/02)
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