Premium
Synthesis and In‐vitro Activity of 4′‐Modified Analogues of ddA as Potent Anti‐HIV Agents
Author(s) -
Hong Joon Hee,
Oh Chang Hyun
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900063
Subject(s) - cytotoxicity , chemistry , ketone , in vitro , stereochemistry , human immunodeficiency virus (hiv) , chemical synthesis , biological activity , combinatorial chemistry , structure–activity relationship , biochemistry , organic chemistry , virology , biology
This paper reports the synthesis of novel 4′‐hydrophobic pocket deoxythreosyl C‐nucleosides. The key threose‐like intermediates 9 and 14 were constructed from acyclic ketone derivatives, respectively. The antiviral activities of the synthesized compounds against the HIV‐1, HSV‐1, HSV‐2, and HCMV viruses were evaluated. The 9‐deaza‐adenine derivatives 10 and 20 showed good anti‐HIV activity without exhibiting significant cytotoxicity.