BISPHOSPHONATE PRODRUGS - SYNTHESIS AND IN-VITRO EVALUATION OF NOVEL PARTIAL AMIDES OF CLODRONIC ACID

Authors
NIEMI R PENNANEN H VEPSALAINEN J TAIPALE H JARVINEN T
Citation
R. Niemi et al., BISPHOSPHONATE PRODRUGS - SYNTHESIS AND IN-VITRO EVALUATION OF NOVEL PARTIAL AMIDES OF CLODRONIC ACID, International journal of pharmaceutics, 174(1-2), 1998, pp. 111-115
Citations number
16
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
International journal of pharmaceutics → ACNP
ISSN journal
03785173
Volume
174
Issue
1-2
Year of publication
1998
Pages
111 - 115
Database
ISI
SICI code
0378-5173(1998)174:1-2<111:BP-SAI>2.0.ZU;2-X
Abstract
Novel partial amides of clodronic acid were synthesized and evaluated in vitro for their properties as bioreversible prodrugs of clodronate. The hydrolysis studies indicated that these derivatives release the p arent drug via chemical hydrolysis. Monoamides were hydrolysed rapidly (t(1/2) = 16-19 min at pH 7.4) to clodronic acid, which suggests that they are useful intermediates in the design of enzymatically labile d ouble prodrugs of clodronate. (C) 1998 Elsevier Science B.V. All right s reserved.