Abstract
We report microwave-assisted synthetic routes, the pharmacokinetic profile along with results from ulcerogenicity and mutagenicity studies of atenolol aspirinate, and an already described derivative, in which acetyl salicylic acid (aspirin®) was connected to atenolol by an ester linkage. Atenolol aspirinate was stable towards aqueous hydrolysis but rapidly hydrolyzed in plasma (t 1/2 = 7.6 min). The results showed that the rapid and complete hydrolysis generates atenolol salicylate, which assumes a conformation stabilized by two intramolecular H-bonds, avoiding its further hydrolysis to salicylic acid and atenolol.
Original language | English (US) |
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Pages (from-to) | 445-455 |
Number of pages | 11 |
Journal | Archiv der Pharmazie |
Volume | 340 |
Issue number | 9 |
DOIs | |
State | Published - Sep 1 2007 |
Keywords
- Antihypertensive therapy
- Atenolol
- Microwave synthesis
- Pharmacokinetics
- Prodrug
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery