基于混合物的杂环组合位置扫描文库：发现对白色念珠菌和新型隐球菌具有强效抗真菌活性的双环胍类化合物。
Mixture-based heterocyclic combinatorial positional scanning libraries: discovery of bicyclic guanidines having potent antifungal activities against Candida albicans and Cryptococcus neoformans.
作者信息
Blondelle S E, Crooks E, Ostresh J M, Houghten R A
机构信息
Torrey Pines Institute for Molecular Studies, San Diego, California 92121, USA.
出版信息
Antimicrob Agents Chemother. 1999 Jan;43(1):106-14. doi: 10.1128/AAC.43.1.106.
Abstract
A mixture-based synthetic combinatorial library of more than 100,000 bicyclic guanidines was generated in a positional scanning format and assayed for activity against Candida albicans. Potent individual bicyclic guanidines were directly identified following the screening of the library. Time-kill curve studies indicated bactericidal activities for the individual bicyclic guanidines. These compounds also showed potent activity against Cryptococcus neoformans. These studies demonstrate the value of using mixture-based combinatorial positional scanning libraries made up of heterocyclic compounds for the rapid identification of novel classes of antifungal compounds.
摘要
构建了一个基于混合物的、包含超过100,000种双环胍的合成组合文库，采用位置扫描形式，并检测其对白色念珠菌的活性。在文库筛选后直接鉴定出了强效的单个双环胍。时间-杀菌曲线研究表明单个双环胍具有杀菌活性。这些化合物对新型隐球菌也显示出强效活性。这些研究证明了使用由杂环化合物组成的基于混合物的组合位置扫描文库来快速鉴定新型抗真菌化合物类别的价值。
相似文献
1
Mixture-based heterocyclic combinatorial positional scanning libraries: discovery of bicyclic guanidines having potent antifungal activities against Candida albicans and Cryptococcus neoformans.基于混合物的杂环组合位置扫描文库：发现对白色念珠菌和新型隐球菌具有强效抗真菌活性的双环胍类化合物。
Antimicrob Agents Chemother. 1999 Jan;43(1):106-14. doi: 10.1128/AAC.43.1.106.
2
Antifungal activity of artemisinin derivatives.青蒿素衍生物的抗真菌活性。
J Nat Prod. 2005 Aug;68(8):1274-6. doi: 10.1021/np050074u.
3
Identification of novel antifungal nonapeptides through the screening of combinatorial peptide libraries based on a hexapeptide motif.通过筛选基于六肽基序的组合肽库鉴定新型抗真菌九肽。
Bioorg Med Chem Lett. 2002 Jun 3;12(11):1473-6. doi: 10.1016/s0960-894x(02)00174-9.
4
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.设计、合成及评估具有强效抗真菌活性的芳香杂环衍生物。
Eur J Med Chem. 2017 Sep 8;137:96-107. doi: 10.1016/j.ejmech.2017.05.043. Epub 2017 May 24.
5
Synthesis, Characterization and Antifungal Evaluation of Novel Thiochromanone Derivatives Containing Indole Skeleton.含吲哚骨架的新型硫代色满酮衍生物的合成、表征及抗真菌活性评价
Chem Pharm Bull (Tokyo). 2016 Sep 1;64(9):1411-6. doi: 10.1248/cpb.c16-00366. Epub 2016 Jul 2.
6
Combinatorial approach to lead optimization of a novel hexapeptide with antifungal activity.一种具有抗真菌活性的新型六肽的先导优化的组合方法。
Bioorg Med Chem Lett. 2000 Aug 21;10(16):1779-81. doi: 10.1016/s0960-894x(00)00343-7.
7
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.联苯咪唑衍生物作为强效抗真菌剂的发现：设计、合成及构效关系研究
Bioorg Med Chem. 2017 Jan 15;25(2):750-758. doi: 10.1016/j.bmc.2016.11.051. Epub 2016 Nov 28.
8
In vitro antifungal and antibiofilm activities of halogenated quinoline analogues against Candida albicans and Cryptococcus neoformans.卤代喹啉类似物对白色念珠菌和新生隐球菌的体外抗真菌和抗生物膜活性。
Int J Antimicrob Agents. 2016 Aug;48(2):208-11. doi: 10.1016/j.ijantimicag.2016.04.019. Epub 2016 May 24.
9
Anti-microbial and anti-biofilm activities of combined chelerythrine-sanguinarine and mode of action against Candida albicans and Cryptococcus neoformans in vitro.联合白屈菜红碱-血根碱的抗微生物和抗生物膜活性及其对体外白色念珠菌和新型隐球菌的作用模式。
Colloids Surf B Biointerfaces. 2020 Jul;191:111003. doi: 10.1016/j.colsurfb.2020.111003. Epub 2020 Apr 1.
10
Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents.苯并噻唑衍生物作为抗真菌剂的设计、合成及构效关系研究。
Eur J Med Chem. 2016 Nov 10;123:514-522. doi: 10.1016/j.ejmech.2016.07.067. Epub 2016 Jul 29.
引用本文的文献
1
Synthesis of Diazacyclic and Triazacyclic Small-Molecule Libraries Using Vicinal Chiral Diamines Generated from Modified Short Peptides and Their Application for Drug Discovery.利用修饰短肽产生的邻位手性二胺合成二氮杂环和三氮杂环小分子文库及其在药物发现中的应用。
Pharmaceuticals (Basel). 2024 Nov 22;17(12):1566. doi: 10.3390/ph17121566.
2
Use of combinatorial library screening to identify inhibitors of a bacterial two-component signal transduction kinase.
Mol Divers. 1998;4(3):173-82. doi: 10.1023/a:1009695718427.
本文引用的文献
1
Comparing individual means in the analysis of variance.方差分析中的个体均值比较。
Biometrics. 1949 Jun;5(2):99-114.
2
The Current Status of Heterocyclic Combinatorial Libraries.杂环组合文库的现状
Chem Rev. 1997 Apr 1;97(2):449-472. doi: 10.1021/cr960010b.
3
Discovery of novel pyridinopolyamines with potent antimicrobial activity: deconvolution of mixtures synthesized by solution-phase combinatorial chemistry.
J Med Chem. 1998 Feb 26;41(5):706-16. doi: 10.1021/jm970598u.
4
Antifungal resistance trends towards the year 2000. Implications for therapy and new approaches.2000年抗真菌耐药性趋势。对治疗的影响及新方法
Drugs. 1997 Nov;54(5):657-78. doi: 10.2165/00003495-199754050-00002.
5
Libraries from libraries: generation and comparison of screening profiles.
Mol Divers. 1996 Oct;2(1-2):41-5. doi: 10.1007/BF01718699.
6
Synthetic peptide combinatorial libraries: a method for the identification of bioactive peptides against phytopathogenic fungi.
Mol Plant Microbe Interact. 1997 Jul;10(5):537-49. doi: 10.1094/MPMI.1997.10.5.537.
7
Antifungal agents: chemotherapeutic targets and immunologic strategies.抗真菌药物：化疗靶点与免疫策略。
Antimicrob Agents Chemother. 1996 Feb;40(2):279-91. doi: 10.1128/AAC.40.2.279.
8
Synthetic combinatorial libraries: novel discovery strategy for identification of antimicrobial agents.合成组合文库：用于鉴定抗菌剂的新型发现策略。
Antimicrob Agents Chemother. 1996 May;40(5):1067-71. doi: 10.1128/AAC.40.5.1067.
9
New and emerging yeast pathogens.新型及新兴酵母病原体
Clin Microbiol Rev. 1995 Oct;8(4):462-78. doi: 10.1128/CMR.8.4.462.
10
Peptide, peptidomimetic, and organic synthetic combinatorial libraries.
Med Res Rev. 1995 Nov;15(6):481-96. doi: 10.1002/med.2610150603.
Zotero 插件