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摘要:
Diketo acid derivatives are potent and selective HIV-1 integrase inhibitors. To investigate the detailed synthesis of those derivatives, a series of p/m-[p-(un)substituted phenylsulfonamidolphenyl beta-diketo acid derivatives have been designed and synthesized. The quinoxalone derivatives as the potential bioisosteres of the biologically labile beta-diketoacid pharmacophores have also been synthesized from reactions of the corresponding diketo acids with o-phenylenediamine. The structures of all diketo acid (ester) and quinoxalone derivatives were confirmed by H-1 NMR, C-13 NMR, IR, HRMS and/or MS (ESI). X-ray crystallographic analysis of 11b demonstrates a similar arrangement of the side chain of quinoxalone derivatives with the parent diketoacids due to the intramolecular hydrogen bond (O center dot center dot center dot H-N) and the sp(2) hybridization configuration of the two nitrogen atoms of the quinoxalone ring.
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来源 :
CHINESE JOURNAL OF CHEMISTRY
ISSN: 1001-604X
年份: 2007
期: 8
卷: 25
页码: 1174-1182
5 . 4 0 0
JCR@2022
ESI学科: CHEMISTRY;
JCR分区:3