From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.

Tozer MJ; Harper EA; Kalindjian SB; Pether MJ; Shankley NP; Watt GF

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From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.

机译：从组胺到咪唑基烷基磺酰胺：一系列新的组胺H3受体拮抗剂的设计。

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Histamine was converted to a selective histamine H3-receptor antagonist by capping the primary amine with 2-naphthalenesulfonyl chloride. Higher receptor affinity and lower variability in the data from the various bioassays were achieved with the 2-naphthalensulfonamides of histamine homologues.

机译：通过用2-萘磺酰氯封端伯胺，将组胺转化为选择性的组胺H3-受体拮抗剂。用组胺同系物的2-萘磺酰胺可以得到较高的受体亲和力和较低的可变性。

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《Bioorganic and Medicinal Chemistry Letters》 |1999年第13期|共6页
作者
Tozer MJ; Harper EA; Kalindjian SB; Pether MJ; Shankley NP; Watt GF;
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正文语种 eng
中图分类药学;生物化学;
关键词
Drug Design; Histamine Antagonists; Imidazoles; Receptors; Histamine H3; 药物设计; 组胺拮抗药; 咪唑类; 受体; 组胺H3; 磺胺类;

机译：Drug Design;Histamine Antagonists;Imidazoles;Receptors;Histamine H3;药物设计;组胺拮抗药;咪唑类;受体;组胺H3;磺胺类;

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1. From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists. [J] . Tozer MJ, Harper EA, Kalindjian SB, Bioorganic and Medicinal Chemistry Letters . 1999,第13期

机译：从组胺到咪唑基烷基磺酰胺：一系列新的组胺H3受体拮抗剂的设计。
2. Synthesis of potent non-imidazole histamine H3-receptor antagonists. [J] . Ganellin CR, Leurquin F, Piripitsi A, Archiv der Pharmazie . 1998,第12期

机译：有效的非咪唑组胺H3受体拮抗剂的合成。
3. Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists. [J] . Kathmann M, Schlicker E, Marr I, Naunyn-Schmiedeberg's Archives of Pharmacology . 1998,第6期

机译：环丙沙星和与化学有关的化合物是高效的选择性组胺H3受体拮抗剂。
4. Rational drug design using mammalian cell lines expressing site-directed mutants of the human H_1 histaminic receptor [C] . Moguilevsky N., Differding E., Gillard M., Annual Meeting of the Japanese Association for Animal Cell Technology . 1998

机译：使用哺乳动物细胞系的理性药物设计表达人H_1组蛋白受体的点定向突变体
5. Novel mechanisms of cardioprotection: Catecholamine release by natriuretic peptides: Characterization and prevention; activation of ALDH2 in mast cell mitochondria: Prevention of local angiotensin II formation; activation of histamine H3-receptors: Reduction of angiotensin AT1-receptor neuronal expression [D] . Chan, Noel Yan-ki 2012

机译：心脏保护的新机制：利钠肽释放儿茶酚胺：表征和预防；肥大细胞线粒体中ALDH2的激活：预防局部血管紧张素II的形成； H3受体的活化：降低血管紧张素AT1受体神经元表达
6. Histamine H1 receptors on adherent rheumatoid synovial cells in culture: demonstration by radioligand binding and inhibition of histamine-stimulated prostaglandin E production by histamine H1 antagonists. [O] . D J Taylor, D E Woolley 1987

机译：培养的类风湿性滑膜细胞上的组胺H1受体：通过放射性配体结合和组胺H1拮抗剂抑制组胺刺激的前列腺素E产生来证明。
7. Binding of histamine H3-receptor antagonists to hematopoietic progenitor cells Evidence for a histamine transporter unrelated to histamine H3 receptors [O] . Corbel Stéphane, Traiffort Elisabeth, Stark Holger, 1997

机译：组胺H3受体拮抗剂与造血祖细胞的结合与组胺H3受体无关的组胺转运蛋白的证据
8. Hyperemia and Edema in the Monkey Spinal Cord Following Injury: Modified by Histamine Antagonists. [R] . Doyle, T. F., Kobrine, A. I., Martins, A. N. 1976

机译：组胺拮抗剂修饰猴脊髓损伤后的充血和水肿。

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.

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