Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors: Latent chirality at N5 in the 1,5-benzodiazepin-2-one nucleus

Tabata H.; Wada N.; Takada Y.; Nakagomi J.; Miike T.; Shirahase H.; Oshitari T.; Takahashi H.; Natsugari H.

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Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors: Latent chirality at N5 in the 1,5-benzodiazepin-2-one nucleus

机译：积极构象的七元环苯并内酰胺类作为新的ACAT抑制剂：1,5-苯并二氮杂-2--2-核中N5的潜在手性

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Nitrogen chirality: Potent new ACAT inhibitors with seven-membered-ring benzolactams as the core structures were first prepared, and the axial chirality recognized by the enzyme was clarified (e.g., 1; see scheme). The chirality at the axis (aS) of 1 controls the conformation of the entire lactam ring, causing the N5-CH _3 to arrange in a pseudo-equatorial position (i.e., the amine at N5 is a chiral center with the S-configuration) both in the crystal state and in solution.

机译：氮手性：首先制备具有七元环苯并内酰胺为核心结构的强力新型ACAT抑制剂，并阐明了该酶识别的轴向手性（例如1;参见方案）。轴（aS）为1的手性控制整个内酰胺环的构象，从而使N5-CH _3排列在伪赤道位置（即，N5处的胺是具有S构型的手性中心）无论是晶体状态还是溶液状态。

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《Chemistry: A European journal》 |2012年第6期|共5页
作者
Tabata H.; Wada N.; Takada Y.; Nakagomi J.; Miike T.; Shirahase H.; Oshitari T.; Takahashi H.; Natsugari H.;
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正文语种 eng
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关键词
atropisomerism; chirality; circular dichroism; lactams; medium-ring compounds;

机译：阻转异构;手性;圆二色性;内酰胺;中环化合物;

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1. Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors: Latent chirality at N5 in the 1,5-benzodiazepin-2-one nucleus [J] . Tabata H., Wada N., Takada Y., Chemistry: A European journal . 2012,第6期

机译：积极构象的七元环苯并内酰胺类作为新的ACAT抑制剂：1,5-苯并二氮杂-2--2-核中N5的潜在手性
2. Elucidation of the Active Conformation of Antiproliferative Sulfonamides, 5N-Arylsulfonyl-1,5-benzodiazepin-2-ones [J] . Tabata Hidetsugu, Funaki Kaoru, Tasaka Tomohiko, The Journal of Organic Chemistry . 2019,第24期

机译：抗增殖磺酰胺，5N-芳基磺酰基-1,5-苯并二氮嘧啶-2-苯并二苯胺的活性构象阐明
3. Conformational studies on plasminogen activator inhibitor (PAI-1) in active, latent, substrate, and cleaved forms. [J] . Sancho E, Declerck PJ, Price NC, Biochemistry . 1995,第3期

机译：纤溶酶原激活物抑制剂（PAI-1）呈活性，潜在，底物和裂解形式的构象研究。
4. Characterization of a Small Molecule Inhibitor of Plasminogen Activator Inhibitor Type 1 That Accelerates the Transition into the Latent Conformation [O] . Ola Fjellström, Johanna Deinum, Tove Sjögren, 2013

机译：纤溶酶原激活剂抑制剂1的小分子抑制剂的表征可加速过渡到潜在构象。
5. Characterization of a Small Molecule Inhibitor of Plasminogen Activator Inhibitor Type 1 That Accelerates the Transition into the Latent Conformation [O] . Ola Fjellström, Johanna Deinum, Tove Sjögren, 2013

机译：纤溶酶原激活剂抑制剂类型1的小分子抑制剂的表征，其将过渡到潜在构象加速

Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors: Latent chirality at N5 in the 1,5-benzodiazepin-2-one nucleus

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