Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.

Scozzafava A; Supuran CT

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Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.

机译：蛋白酶抑制剂：合并磺酰基-L-丙氨酸异羟肟酸酯部分的溶组织梭状芽孢杆菌胶原酶抑制剂的合成。

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A series of hydroxamates was obtained by the reaction of N-(4-nitrobenzyl)-L-alanine with alkyl/arylsulfonyl halides, followed by conversion of the COOH group into CONHOH. Structurally-related compounds were prepared similarly by using arylsulfonyl isocyanates, aryl isocyanates or arylsulfenyl halides instead of the sulfonyl halides. Many of the new compounds showed nanomolar affinity for the bacterial collagenase isolated from the pathogen Clostridium histolyticum.

机译：通过使N-（4-硝基苄基）-L-丙氨酸与烷基/芳基磺酰基卤化物反应，然后将COOH基团转化为CONHOH，获得一系列异羟肟酸酯。通过使用芳基磺酰基异氰酸酯，芳基异氰酸酯或芳基亚磺酰基卤化物代替磺酰基卤化物类似地制备与结构相关的化合物。许多新化合物对从病原梭状芽胞杆菌分离的细菌胶原酶表现出纳摩尔亲和力。

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《Bioorganic and Medicinal Chemistry Letters》 |2000年第5期|共4页
作者
Scozzafava A; Supuran CT;
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正文语种 eng
中图分类药学;生物化学;
关键词
Alanine; Hydroxamic Acids; Microbial Collagenase; Protease Inhibitors; 丙氨酸; 羟肟酸类; 微生物胶原酶; 蛋白酶抑制药;

机译：Alanine;Hydroxamic Acids;Microbial Collagenase;Protease Inhibitors;丙氨酸;羟肟酸类;微生物胶原酶;蛋白酶抑制药;

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1. Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties. [J] . Scozzafava A, Supuran CT Bioorganic and Medicinal Chemistry Letters . 2000,第5期

机译：蛋白酶抑制剂：合并磺酰基-L-丙氨酸异羟肟酸酯部分的溶组织梭状芽孢杆菌胶原酶抑制剂的合成。
2. Protease inhibitors: synthesis of bacterial collagenase and matrix metalloproteinase inhibitors incorporating succinyl hydroxamate and iminodiacetic acid hydroxamate moieties. [J] . Santos MA, Marques S, Gil M, Journal of enzyme inhibition and medicinal chemistry. . 2003,第3期

机译：蛋白酶抑制剂：合成细菌胶原酶和基质金属蛋白酶抑制剂，其掺入琥珀酰羟肟酸甲酯和亚单乙酸羟胺部分。
3. Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties. [J] . Scozzafava A, Supuran CT Journal of Medicinal Chemistry . 2000,第9期

机译：蛋白酶抑制剂：结合N-4-硝基苄基磺酰基甘氨酸异羟肟酸酯部分的有效细菌胶原酶和基质金属蛋白酶抑制剂的合成。
4. Novel Protease Inhibitor Inhibiting Proliferation of Influenza Virus: Purification and cDNA Cloning of a Novel Protease Inhibitor Secreted by MDCK Cells [C] . Kiyoto Nishiyama, Keishin Sugawara, Kenji Soejima, Annual and International Meeting of the Japanese Association for Animal Cell Technology . 2010

机译：抑制流感病毒的新型蛋白酶抑制剂：用MDCK细胞分泌的新型蛋白酶抑制剂的纯化和cDNA克隆
5. Design and synthesis of core structural intermediates for novel HIV-1 protease inhibitors and synthesis, biological activity and molecular modeling of novel 20S proteasome inhibitors. [D] . Avancha, Kiran Kumar Venkata Raja. 2006

机译：新型HIV-1蛋白酶抑制剂的核心结构中间体的设计与合成，新型20S蛋白酶体抑制剂的合成，生物学活性和分子建模。
6. Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: synthesis biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex [O] . Arun K. Ghosh, Margherita Brindisi, Prasanth R. Nyalapatla, -1

机译：包含间苯二甲酰胺衍生的P2-P3配体的新型HIV-1蛋白酶抑制剂的设计：抑制剂-HIV-1蛋白酶复合物的合成生物学评估和X射线结构研究
7. Protease Inhibitors: Synthesis of Bacterial Collagenase and Matrix Metalloproteinase Inhibitors Incorporating Succinyl Hydroxamate and Iminodiacetic Acid Hydroxamate Moieties [O] . M. Amélia Santos, Sérgio Marques, Marco Gil, 2003

机译：蛋白酶抑制剂：合成细菌胶原酶和基质金属蛋白酶抑制剂，其掺入琥珀酸羟肟酸酯和亚单乙酸羟肟酸羟肟酸酯部分

Protease inhibitors: synthesis of clostridium histolyticum collagenase inhibitors incorporating sulfonyl-L-alanine hydroxamate moieties.

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