SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

Zhou G; Ting PC; Aslanian R; Cao J; Kim DW; Kuang R; Lee JF; Schwerdt J; Wu H; Herr RJ; Zych AJ; Yang J; Lam S; Wainhaus S; Black TA; McNicholas PM; Xu Y; Walker SS

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SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

机译：SAR研究哒嗪酮衍生物作为新型葡聚糖合成酶抑制剂。

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A novel series of pyridazinone analogs has been developed as potent beta-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one (1). The effect of changes to the core structure is described in detail. Optimization of the sulfonamide moiety led to the identification of important compounds with much improved systematic exposure while retaining good antifungal activity against the fungal strains Candida glabrata and Candida albicans.

机译：通过引线5- [4-（苄基磺酰基）哌嗪-1-基] -4-morpholino-2-的结构 - 活性关系研究，开发了一种新颖的哒嗪酮类似物作为有效的β-1,3-葡聚糖合成酶抑制剂。-4-morpholino-2- 苯基 - 哒嗪-3（2H） - ONE（1）。详细描述了对核心结构的改变的影响。磺胺酰胺部分的优化导致鉴定具有大大改进的系统曝光的重要化合物，同时保持对真菌菌株的良好抗真菌活性念珠菌念珠菌和念珠菌念珠菌。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共4页
作者
Zhou G; Ting PC; Aslanian R; Cao J; Kim DW; Kuang R; Lee JF; Schwerdt J; Wu H; Herr RJ; Zych AJ; Yang J; Lam S; Wainhaus S; Black TA; McNicholas PM; Xu Y; Walker SS;
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Department of Chemical Research Merck Research Laboratories 2015 Galloping Hill Road Kenilworth NJ 07033 USA.;

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正文语种 eng
中图分类药学;
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1. SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors. [J] . Zhou G, Ting PC, Aslanian R, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：SAR研究哒嗪酮衍生物作为新型葡聚糖合成酶抑制剂。
2. Multivariate SAR/QSAR of 3-aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase (FAS) inhibitors. [J] . de Melo EB European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第12期

机译：3-芳基-4-羟基喹啉-2（1H）-one衍生物作为I型脂肪酸合酶（FAS）抑制剂的多元SAR / QSAR。
3. Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors [J] . ZychA.J., LamS.Q., JenkinsD.M., Bioorganic and Medicinal Chemistry Letters . 2012,第14期

机译：基于磺酰脲类哌嗪哒嗪酮系列的葡聚糖合成酶抑制剂铅优化
4. Rational Design, Synthesis and SAR Study of Some Cyclopropane Derivatives as KARI Inhibitors [C] . Li Jiusheng, rnZhao Xiaoli, rnKang Yanlong Proceedings of the 3rd International Symposium on Pesticide and Environmental Safety amp; 7th International Workshop on Crop Protection Chemistry and Regulatory Harmonization . 2007

机译：某些环丙烷衍生物作为KARI抑制剂的合理设计，合成和SAR研究
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Identification of the FKS1 gene of Candida albicans as the essential target of 13-beta-D-glucan synthase inhibitors. [O] . C M Douglas, J A DIppolito, G J Shei, 1997

机译：鉴定白色念珠菌的FKS1基因为13-β-D-葡聚糖合酶抑制剂的基本靶标。
7. Docking and quantitative structure-activity relationship of bi-cyclic heteroaromatic pyridazinone and pyrazolone derivatives as phosphodiesterase 3A (PDE3A) inhibitors. [O] . Camila Muñoz-Gutiérrez, Daniela Cáceres-Rojas, Francisco Adasme-Carreño, 2017

机译：双环杂芳基哒嗪酮和吡唑啉酮衍生物作为磷酸二酯酶3a（pDE3a）抑制剂的对接和定量构效关系。

SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.

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