Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment

被引:38
作者
Andrews, Katherine T. [1 ,2 ]
Fisher, Gillian M. [1 ,2 ]
Sumanadasa, Subathdrage D. M. [1 ,2 ]
Skinner-Adams, Tina [1 ,2 ]
Moeker, Janina [1 ]
Lopez, Marie [1 ]
Poulsen, Sally-Ann [1 ]
机构
[1] Griffith Univ, Eskitis Inst Drug Discovery, Nathan, Qld 4111, Australia
[2] Queensland Inst Med Res, Herston, Qld 4029, Australia
基金
澳大利亚研究理事会; 英国医学研究理事会;
关键词
Sulfonamide; Primary sulfonamide; Antimalarial; Plasmodium falciparum; SAR; Carbonic anhydrase; ARTEMISININ-RESISTANT MALARIA; CARBONIC-ANHYDRASE INHIBITORS; IN-VITRO; SERUM-ALBUMIN; XII; IX;
D O I
10.1016/j.bmcl.2013.09.015
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
Despite the urgent need for effective antimalarial drugs with novel modes of action no new chemical class of antimalarial drug has been approved for use since 1996. To address this, we have used a rational approach to investigate compounds comprising the primary benzene sulfonamide fragment as a potential new antimalarial chemotype. We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds. Our findings provide a platform to support the further evaluation of primary benzene sulfonamides as a new antimalarial chemotype, including the identification of the target of these compounds in the parasite. (c) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6114 / 6117
页数:4
相关论文
共 22 条
[1]
Click Chemistry beyond Metal-Catalyzed Cycloaddition [J].
Becer, C. Remzi ;
Hoogenboom, Richard ;
Schubert, Ulrich S. .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2009, 48 (27) :4900-4908
[2]
Capasso C., 2013, ENZYME INHIB MED CHE
[3]
Anti-infective carbonic anhydrase inhibitors: a patent and literature review [J].
Capasso, Clemente ;
Supuran, Claudiu T. .
EXPERT OPINION ON THERAPEUTIC PATENTS, 2013, 23 (06) :693-704
[4]
Synthesis of acylated glycoconjugates as templates to investigate in vitro biopharmaceutical properties [J].
Carroux, Cindy J. ;
Moeker, Janina ;
Motte, Josephine ;
Lopez, Marie ;
Bornaghi, Laurent F. ;
Katneni, Kasiram ;
Ryan, Eileen ;
Morizzi, Julia ;
Shackleford, David M. ;
Charman, Susan A. ;
Poulsen, Sally-Ann .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (02) :455-459
[5]
Esterase activity of bovine serum albumin up to 160°C:: A new benchmark for biocatalysis [J].
Cordova, Jesus ;
Ryan, Jessica D. ;
Boonyaratanakornkit, Boonchai B. ;
Clark, Douglas S. .
ENZYME AND MICROBIAL TECHNOLOGY, 2008, 42 (03) :278-283
[6]
Artemisinin resistance: current status and scenarios for containment [J].
Dondorp, Arjen M. ;
Yeung, Shunmay ;
White, Lisa ;
Nguon, Chea ;
Day, Nicholas P. J. ;
Socheat, Duong ;
von Seidlein, Lorenz .
NATURE REVIEWS MICROBIOLOGY, 2010, 8 (04) :272-280
[7]
Artemisinin Resistance in Plasmodium falciparum Malaria. [J].
Dondorp, Arjen M. ;
Nosten, Francois ;
Yi, Poravuth ;
Das, Debashish ;
Phyo, Aung Phae ;
Tarning, Joel ;
Lwin, Khin Maung ;
Ariey, Frederic ;
Hanpithakpong, Warunee ;
Lee, Sue J. ;
Ringwald, Pascal ;
Silamut, Kamolrat ;
Imwong, Mallika ;
Chotivanich, Kesinee ;
Lim, Pharath ;
Herdman, Trent ;
An, Sen Sam ;
Yeung, Shunmay ;
Singhasivanon, Pratap ;
Day, Nicholas P. J. ;
Lindegardh, Niklas ;
Socheat, Duong ;
White, Nicholas J. .
NEW ENGLAND JOURNAL OF MEDICINE, 2009, 361 (05) :455-467
[8]
In vitro evaluations of antimalarial drugs and their relevance to clinical outcomes [J].
Ekland, Eric H. ;
Fidock, David A. .
INTERNATIONAL JOURNAL FOR PARASITOLOGY, 2008, 38 (07) :743-747
[9]
Kerns E. H., 2008, DRUG LIKE PROPERTIES, P260
[10]
Practical aspects of the ligand-binding and enzymatic properties of human serum albumin [J].
Kragh-Hansen, U ;
Chuang, VTG ;
Otagiri, M .
BIOLOGICAL & PHARMACEUTICAL BULLETIN, 2002, 25 (06) :695-704