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Synthesis and biological evaluation of novel tert-azido or ten-amino substituted penciclovir analogs

Title
Synthesis and biological evaluation of novel tert-azido or ten-amino substituted penciclovir analogs
Authors
Kim H.O.Baek H.W.Moon H.R.Kim D.-K.Chun M.W.Jeong L.S.
Ewha Authors
정낙신김대기
SCOPUS Author ID
김대기scopus
Issue Date
2004
Journal Title
Organic and Biomolecular Chemistry
ISSN
1477-0520JCR Link
Citation
Organic and Biomolecular Chemistry vol. 2, no. 8, pp. 1164 - 1168
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
tert-Azido or amino substituted penciclovir analogs, 1-3 were synthesized for the purpose of improving the efficacy and bioavailability of penciclovir and searching for novel antiviral agents. Among several methods attempted to insert an azido group into the α,β-unsaturated ester 6, only Brønsted acid-catalysed 1,4-conjugate addition conditions (NaN 3, 75% acetic acid, 80°C) gave the desired tert-azido product 7. The synthesized final penciclovir analogs 1-3 were evaluated in vitro against several viruses such as HIV-1, HSV-1 and 2, poliovirus, VZV, and VSV. Compound 2 only showed weak antiviral activity against HSV-1 without cytotoxicity. Although the synthesized compounds did not exhibit an excellent antiviral activity, the successful method used in introducing the tert-azido group is expected to be generally utilized for the synthesis of nucleoside analogs with a tert-azido substituent.
DOI
10.1039/b401100g
Appears in Collections:
약학대학 > 약학과 > Journal papers
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