Bioorganic and Medicinal Chemistry Letters, volume 20, issue 22, pages 6644-6648
Bromophenols as Candida albicans isocitrate lyase inhibitors
Ki-Bong Oh
1
,
Heung Jeon
2
,
Yu Ri Han
3
,
Yeon Ju Lee
3
,
Jiyoung Park
1
,
So-Hyoung Lee
1
,
Dongsik Yang
2
,
Mihyun Kwon
2
,
Jongheon Shin
4
,
Hyi-Seung Lee
3
3
Marine Natural Products Laboratory, Korea Ocean Research & Development Institute, Ansan PO Box 29, Seoul 425-600, Republic of Korea
|
Publication type: Journal Article
Publication date: 2010-11-01
scimago Q2
SJR: 0.508
CiteScore: 5.7
Impact factor: 2.5
ISSN: 0960894X, 14643405
PubMed ID:
20888765
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The synthesis and bioactivity of bromophenols are described. A new series of bromophenols was synthesized by reactions of corresponding phenol analogs with bromine. The synthesized compounds were tested for inhibitory activity against isocitrate lyase (ICL) of Candida albicans and antimicrobial activity against Gram-positive and, Gram-negative bacteria and fungi. Among the synthesized bromophenols, bis(3-bromo-4,5-dihydroxyphenyl)methanone ( 11 ) and (3-bromo-4,5-dihydroxyphenyl)(2,3-dibromo-4,5-dihydroxyphenyl)methanone ( 12 ) displayed potent inhibitory activities against ICL, showing a stronger inhibitory effects than were found with natural bromophenol 1 . The preliminary structure–activity relationships were investigated in order to determine the essential structural requirements for the inhibitory activities of these compounds against ICL of C. albicans .
Found
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.