Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.

Kummerle AE; Raimundo JM; Leal CM

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Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.

机译：关于鉴定有效的血管扩张剂亚芳基N-酰基hydr衍生物的假定生物活性构象的研究。

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In this report we disclose the synthesis, vasodilatory activity, and identification of bioactive conformation of new N-acylhydrazone and N-methyl-N-acylhydrazone derivatives, structurally designed by bioisosteric replacements of previously described cardioactive compounds LASSBio-294 and its N-methyl derivative LASSBio-785. Some of these novel derivatives presented improved vasorelaxant properties, being new cardiovascular drug candidates.

机译：在本报告中，我们披露了新的N-酰基hydr和N-甲基-N-酰基hydr衍生物的合成，血管舒张活性和生物活性构象的鉴定，这些衍生物的结构是通过对上述心脏活性化合物LASSBio-294及其N-甲基衍生物进行生物等位替代而设计的LASSBio-785。这些新颖的衍生物中的一些表现出改善的血管舒张性质，是新的心血管药物候选物。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第10期|共6页
作者
Kummerle AE; Raimundo JM; Leal CM;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives. [J] . Kummerle AE, Raimundo JM, Leal CM European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第10期

机译：关于鉴定有效的血管扩张剂亚芳基N-酰基hydr衍生物的假定生物活性构象的研究。
2. Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors [J] . Kümmerle A.E., Schmitt M., Cardozo S.V.S., Journal of Medicinal Chemistry . 2012,第17期

机译：N-酰基hydr和新型构象受限化合物作为选择性和有效的口服活性磷酸二酯酶-4抑制剂的设计，合成和药理评估
3. Characterization of the conformational ensemble from bioactive N-acylhydrazone derivatives [J] . Pol-Fachin L, Fraga CAM, Barreiro EJ, Journal of molecular graphics & modelling . 2010,第5期

机译：生物活性N-酰基hydr衍生物的构象集合的表征
4. Exploration of conformational space of linear EAE antagonist Arg~(91), Ala~(96) MBP_(87-99) and proposal of a putative bioactive conformation in DMSO-d_6 [C] . E. D. Mantzourani, T. V. Tselios, S. Golic-Grdadolnik, Advances in Computational Methods in Sciences and Engineering 2005 vol.4A; Lecture Series on Computer and Computational Sciences; vol.4A . 2005

机译：线性EAE拮抗剂Arg〜（91），Ala〜（96） MBP_（87-99）的构象空间探索及在DMSO-d_6中推测的生物活性构象的建议
5. BIOCHEMICAL STUDY OF POLY-ALPHA-L-GLUTAMIC ACID. PART I: THE EFFECT OF CONFORMATION ON THE CHEMICAL, PEPSIN OR PRONASE HYDROLYSIS OF POLY-ALPHA-L-GLUTAMIC ACID. PART II: BIOLOGICAL PROPERTIES OF POLY-ALPHA-L- GLUTAMIC ACID AND ITS DERIVATIVES. PART III: A NEW CALCIUM REQUIREMENT FOR THE HYDROLYSIS OF POLY-ALPHA-L-GLUTAMIC ACID BY THE CULTURE FILTRATESFROM BACILLUS LICHINOFORMIS. [D] . WAGLE, SUDHAKAR SHANTARAM. 1965

机译：聚α-L-谷氨酸的生物化学研究。第一部分：构象对聚-α-L-谷氨酸酸的化学，胃蛋白酶或蛋白酶水解的影响。第二部分：聚α-L-谷氨酸及其衍生物的生物学特性。第三部分：新的钙要求，用于培养滤液中的嗜酸芽孢杆菌（BACILLUS LICHINOFORMIS）水解聚-α-L-谷氨酸。
6. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501 a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases [O] . Franz von Nussbaum, Volkhart M-J Li, Swen Allerheiligen, -1

机译：冻结生物活性构象以增强效能：BAY 85-8501的鉴定BAY 85-8501是人类中性粒细胞弹性蛋白酶对肺部疾病的选择性和强效抑制剂
7. Cover Picture: Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases (ChemMedChem 7/2015) [O] . Franz von Nussbaum, Volkhart M.-J. Li, Swen Allerheiligen, 2015

机译：封面图片：冻结生物活性构象以提高效力：肺病85-8501的鉴定，肺部疾病的人性化粒细胞弹性蛋白酶的选择性和有效抑制剂（ChemMedchem 7/2015）
8. Conformational Study of Jet-Cooled Styrene Derivatives. Demonstration of the Planarity of Non-Sterically Hindered Styrenes [R] . Grassian, V. H., Bernstein, E. R., Secor, H. V., 1989

机译：喷射冷却苯乙烯衍生物的构象研究。非空间位阻苯乙烯平面性的证明

Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.

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