Improvement of the absorption of oral (R,S)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine, an anti-varicella-zoster virus drug, in rats and monkeys | Zendy

Desmond M. LakeBakaar | Zendy; B Lindborg | Zendy; R. Datema | Zendy

Open Access

Improvement of the absorption of oral (R,S)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine, an anti-varicella-zoster virus drug, in rats and monkeys

Author(s) -

Desmond M. LakeBakaar,

B Lindborg,

R. Datema

Publication year - 1989

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.33.1.110

Subject(s) - hydroxymethyl , prodrug , guanine , bioavailability , absorption (acoustics) , hydrochloride , pharmacokinetics , chemistry , in vivo , drug , pharmacology , oral administration , stereochemistry , medicine , biochemistry , biology , nucleotide , physics , microbiology and biotechnology , acoustics , gene

In an effort to improve the gastrointestinal absorption of (R,S)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine [(+/-)2HM-HBG], various salts and esters of the compound were synthesized and pharmacokinetic experiments were performed in rats and monkeys. The sodium or hydrochloride salts and short-chain esters of (+/-)2HM-HBG showed bioavailability characteristics that were equally as poor as those of (+/-)2HM-HBG. However, the esters given as salts tended to be better absorbed than the parent compound. The 6-deoxy and 6-deoxydiacetate analogs were extensively oxidized in vivo and represent prodrugs with considerable potential in improving the absorption of oral (+/-)2HM-HBG.

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