Optically active iodohelicene derivatives exhibit histamine N-methyl transferase inhibitory activity

Ichinose Wataru; Sawato Tsukasa; Kitano Haruna; Shinozaki Yasuhiro; Arisawa Mieko; Saito Nozomi; Yoshikawa Takeo; Yamaguchi Masahiko

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Optically active iodohelicene derivatives exhibit histamine N-methyl transferase inhibitory activity

机译：光学活性碘丙烯衍生物表现出组胺N-甲基转移酶抑制活性

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Optically active helicene derivatives inhibit the activity on histamine N-methyl transferase (HNMT). Specifically, methyl (P)-1,12-dimethylbenzoMphenanthrene-8-carboxylate with 6-iodo and 5-trifluoromethanesulfonyloxy groups inhibits HNMT activity on the mu M order of IC50. Chirality is important, and (M)-isomers exhibits substantially reduced activity. The 6-iodo group is also essential, which suggests the involvement of halogen bonds in protein binding. Substituents on the sulfonate moiety also affect the inhibitory activity.

机译：光学活性甲丙烯衍生物抑制组胺N-甲基转移酶（HNMT）上的活性。具体地，甲基（P）-1,12-二甲基苯苯蒽蒽-8-羧酸甲酯，具有6-碘和5-三氟甲磺酰氧基抑制了IC50的MU M级上的HNMT活性。手性是重要的，（M） - 异构体表现出显着减少的活性。 6-Iodo组也是必不可少的，这表明卤素键参与蛋白质结合。磺酸盐部分上的取代基也影响抑制活性。

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《The Journal of Antibiotics: An International Journal》 |2019年第6期|共6页
作者
Ichinose Wataru; Sawato Tsukasa; Kitano Haruna; Shinozaki Yasuhiro; Arisawa Mieko; Saito Nozomi; Yoshikawa Takeo; Yamaguchi Masahiko;
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Tohoku Univ Grad Sch Pharmaceut Sci Dept Organ Chem Aoba Ku Sendai Miyagi 9808578 Japan;

Tohoku Univ Grad Sch Pharmaceut Sci Dept Organ Chem Aoba Ku Sendai Miyagi 9808578 Japan;

Tohoku Univ Grad Sch Med Dept Pharmacol Aoba Ku Sendai Miyagi 9808575 Japan;

Tohoku Univ Grad Sch Pharmaceut Sci Dept Organ Chem Aoba Ku Sendai Miyagi 9808578 Japan;

Tohoku Univ Grad Sch Pharmaceut Sci Dept Organ Chem Aoba Ku Sendai Miyagi 9808578 Japan;

Tohoku Univ Grad Sch Med Dept Pharmacol Aoba Ku Sendai Miyagi 9808575 Japan;

Tohoku Univ Grad Sch Pharmaceut Sci Dept Organ Chem Aoba Ku Sendai Miyagi 9808578 Japan;

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正文语种 eng
中图分类药学;
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1. Optically active iodohelicene derivatives exhibit histamine N-methyl transferase inhibitory activity [J] . Ichinose Wataru, Sawato Tsukasa, Kitano Haruna, The Journal of Antibiotics: An International Journal . 2019,第6期

机译：光学活性碘丙烯衍生物表现出组胺N-甲基转移酶抑制活性
2. In-Silico Pharmacodynamics: Correlation of Adverse Effects of H2-Antihistamines with Histamine N-Methyl Transferase Binding Potential [J] . Vinod P K, Konkimalla Badireenath, Chandra Nagasuma Applied bioinformatics . 2006,第3期

机译：硅内药效学：H2-抗组胺药与组胺N-甲基转移酶结合潜能的不良影响相关
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4. Synthesis of uronic acid derivatives with unsaturated bond andtheir infection inhibitory activity against Japanese encephalitis virus [C] . Reo Kondo, Kazuya I.P.J.Hidari, Hirofumi Nakano 日本化学会春季年会 . 2020

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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. Histamine N-methyl transferase: inhibition by drugs. [O] . G M Pacifici, P Donatelli, L Giuliani 1992

机译：组胺N-甲基转移酶：被药物抑制。
7. Histamine N-methyl transferase: inhibition by drugs. [O] . Pacifici, G M, Donatelli, P, Giuliani, L 1992

机译：组胺N-甲基转移酶：被药物抑制。

Optically active iodohelicene derivatives exhibit histamine N-methyl transferase inhibitory activity

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