CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIPS OF PYRIPYROPENES .3. SYNTHETIC CONVERSION OF PYRIDINE-PYRONE MOIETY

Obata R.; Tian ZM.; Tomoda H.; Harigaya Y.; Omura S.; Sunazuka T.

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CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIPS OF PYRIPYROPENES .3. SYNTHETIC CONVERSION OF PYRIDINE-PYRONE MOIETY

机译：吡咯烷酮的化学改性和结构-活性关系.3。吡啶-吡喃部分的合成转化

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Structure-activity relationships of the pyridine-pyrone moiety in pyripyropene A (1), a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor of fungal origin, were studied. Several kinds of aromatic or hetero ring substituents for the pyridine moiety were synthesized using unique degradation reaction, following by gamma-acylation. All the six synthesized analogs decreased the inhibitory activity with 20 to 200 times larger IC50 values than that of 1. Furthermore, the pyridine-pyrone substituent also dramatically decrease the inhibitory activity. Thus, the pyridine-pyrone moiety is important for eliciting potent ACAT inhibition. [References: 11]

机译：研究了吡啶并戊二烯A（1）中的吡啶-吡喃酮部分的结构活性关系，吡啶并吡喃酮A是一种有效的真菌来源的酰基CoA：胆固醇酰基转移酶（ACAT）抑制剂。使用独特的降解反应，然后进行γ-酰化反应，合成了吡啶部分的几种芳族或杂环取代基。所有六个合成的类似物均降低了抑制活性，其IC50值是其1的20到200倍。此外，吡啶-吡喃酮取代基也显着降低了抑制活性。因此，吡啶-吡喃酮部分对于引起有效的ACAT抑制是重要的。 [参考：11]

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来源
《The Journal of Antibiotics: An International Journal》 |1997年第3期|共8页
作者
Obata R.; Tian ZM.; Tomoda H.; Harigaya Y.; Omura S.; Sunazuka T.;
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原文格式 PDF
正文语种 eng
中图分类药学;药品;
关键词
Acyl-coa; Inhibitors; Potent;

机译：酰基可可;抑制剂;有效;

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1. CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIPS OF PYRIPYROPENES .3. SYNTHETIC CONVERSION OF PYRIDINE-PYRONE MOIETY [J] . Obata R., Tian ZM., Tomoda H., The Journal of Antibiotics: An International Journal . 1997,第3期

机译：吡咯烷酮的化学改性和结构-活性关系.3。吡啶-吡喃部分的合成转化
2. Structure-activity relationships study of pyripyropenes: Reversal of cancer cell multidrug resistance [J] . Obata R., Harigaya Y., Hayashi M., The Journal of Antibiotics: An International Journal . 2000,第4期

机译：吡咯烷的构效关系研究：癌细胞多药耐药性的逆转
3. Structure-activity relationship for adenosine kinase from Mycobacterium tuberculosis II. Modifications to the ribofuranosyl moiety. [J] . Long MC, Shaddix SC, Moukha-Chafiq O, Biochemical Pharmacology . 2008,第8期

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4. Synthesis, antigenicity against human sera and structure-activity relationships of carbohydrate moiety from Toxocara Larvae and its analogues [C] . N. Hada, A. Koizumi, T. Tsuchiya International Carbohydrate Symposium . 2013

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5. Side Chain Modifications to Improve Peptide Structure-Activity Relationships [D] . Lahankar, Neelam 2018

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6. Extensive CRISPR RNA modification reveals chemical compatibility and structure-activity relationships for Cas9 biochemical activity [O] . Daniel O’Reilly, Zachary J Kartje, Eman A Ageely, 2019

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7. Structure-activity Relationships Study of Pyripyropenes. Reversal of Cancer Cell Multidrug Resistance. [O] . RIKA OBATA, TOSHIAKI SUNAZUKA, YOSHIHIRO HARIGAYA, 2000

机译：吡吡化胶的结构 - 活性关系研究。逆转癌细胞多药耐药性。
8. Structure-Activity Relationships for the Degradation of a Mixture of Organic Chemicals in Soil [R] . Anderson, T. A. , Walton, B. T. 1989

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CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY RELATIONSHIPS OF PYRIPYROPENES .3. SYNTHETIC CONVERSION OF PYRIDINE-PYRONE MOIETY

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