| Literature DB >> 17560110 |
Takashi Kawasuji1, Masahiro Fuji, Tomokazu Yoshinaga, Akihiko Sato, Tamio Fujiwara, Ryuichi Kiyama.
Abstract
The two-metal binding model we previously reported as an inhibition mechanism of HIV integrase (HIV IN) produced a new direction in modification of 2-hydroxy-3-heteroaryl acrylic acid inhibitors (HHAAs). Here we present a novel series of HIV IN inhibitors having a 3-hydroxy-1,5-dihydro-pyrrol-2-one moiety (HDPO) as an advanced analog of HHAAs. This cyclic modification of the chelating region of HHAA produces a favorable configuration to coordinate two-metal ions in HIV IN, which consequently gave improvements in not only enzymatic assay but also antiviral cell based assay in many cases.Entities:
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Year: 2007 PMID： 17560110 DOI： 10.1016/j.bmc.2007.05.052
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641