1.
Bioorg Med Chem
; 16(10): 5788-94, 2008 May 15.
Article
in English
| MEDLINE
| ID: mdl-18434167
ABSTRACT
In this work we prepared and characterized an inclusion complex of the dihydropteroate synthase inhibitor sulfadiazine (SDZ) in 2-hydroxypropyl-beta-cyclodextrin (HPBCD). From the phase-solubility diagram we observed an increase in the water solubility of the drug, calculating a binding constant of 1879M(-1). The inclusion mode involves a NH(2)-in orientation of the drug in the HPBCD cavity, according to the 2D NMR (ROESY) data and confirmed by molecular modeling using the semiempirical PM6 and RM1 methods.
Subject(s)
Enzyme Inhibitors/chemical synthesis , Sulfadiazine/chemistry , beta-Cyclodextrins/chemistry , 2-Hydroxypropyl-beta-cyclodextrin , Chemical Phenomena , Chemistry, Physical , Dihydropteroate Synthase/antagonists & inhibitors , Drug Carriers/chemistry , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Magnetic Resonance Spectroscopy/methods , Models, Molecular , Molecular Structure , Phase Transition , Solubility , Structure-Activity Relationship , Temperature , Water/chemistry , X-Ray Diffraction
2.
s.l; s.n; 1993. 8 p. ilus, tab.
Non-conventional
in English
| Sec. Est. Saúde SP, HANSEN, Hanseníase Leprosy, SESSP-ILSLACERVO, Sec. Est. Saúde SP
| ID: biblio-1236777