Orally active PDE4 inhibitors with therapeutic potential.

Ochiai H; Ohtani T; Ishida A; Kishikawa K; Obata T; Nakai H; Toda M

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Orally active PDE4 inhibitors with therapeutic potential.

机译：具有治疗潜力的口服活性PDE4抑制剂。

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Based on the successful results in the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid moiety, nitrile moiety and 3-cyclopentyl-4-methoxyphenyl moiety) in the structure of Ariflo 1 was attempted using a bicyclo[3.3.0]octane template instead of a cyclohexane template. As a result, 2a, 7a and 7b were found to be orally active and were predicted to have an improved therapeutic potential based on evaluation by cross-species and same-species comparisons. Structure-activity relationships (SARs) of these compounds are also discussed.

机译：根据Ariflo临床试验的成功结果，尝试使用双环化合物进一步优化Ariflo 1结构中三个药效团（羧酸部分，腈部分和3-环戊基-4-甲氧基苯基部分）的空间排列用[3.3.0]辛烷模板代替环己烷模板。结果，基于跨物种和同物种比较的评估，发现2a，7a和7b具有口服活性并且被预测具有改善的治疗潜力。还讨论了这些化合物的构效关系（SAR）。

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《Bioorganic and Medicinal Chemistry Letters》 |2004年第5期|共5页
作者
Ochiai H; Ohtani T; Ishida A; Kishikawa K; Obata T; Nakai H; Toda M;
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原文格式 PDF
正文语种 eng
中图分类基础医学;
关键词
Therapeutic; Ariflo; inhibitors; structure; pharmacophore;

机译：治疗性;Ariflo;抑制剂;结构;药效团;

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专利

1. New orally active PDE4 inhibitors with therapeutic potential. [J] . Ochiai H, Ishida A, Ohtani T, Bioorganic and medicinal chemistry . 2004,第15期

机译：具有治疗潜力的新型口服活性PDE4抑制剂。
2. Orally active PDE4 inhibitors with therapeutic potential. [J] . Ochiai H, Ohtani T, Ishida A, Bioorganic and Medicinal Chemistry Letters . 2004,第5期

机译：具有治疗潜力的口服活性PDE4抑制剂。
3. Orally active PDE4 inhibitor with therapeutic potential. [J] . Ochiai H, Ohtani T, Ishida A, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2004,第7期

机译：具有治疗潜力的口服活性PDE4抑制剂。
4. Identification of therapeutic inhibitors for the treatment of oral cancer using herbal bio-active principles by means of computational approach [C] . P L. Sujatha, Ravi Reddy, Jaideep Mahendra, International Conference on Advances in Electrical, Electronics, Information, Communication and Bio-Informatics . 2016

机译：利用草药生物活性原理通过计算方法鉴定治疗口腔癌的治疗抑制剂
5. Synthesis of boronic acid based sensors for glucose and sialic acid and synthesis of novel and selective PDE4 enzyme inhibitors. [D] . Kaur, Gurpreet. 2006

机译：合成基于硼酸的葡萄糖和唾液酸传感器，以及合成新型选择性PDE4酶抑制剂。
6. Dual inhibition of angiotensin-converting enzyme and neutral endopeptidase by the orally active inhibitor mixanpril: a potential therapeutic approach in hypertension. [O] . M C Fournié-Zaluski, W Gonzalez, S Turcaud, 1994

机译：口服活性抑制剂mixanpril对血管紧张素转化酶和中性内肽酶的双重抑制：高血压的一种潜在治疗方法。
7. The effect of a novel orally active selective PDE4 isoenzyme inhibitor (CDP840) on allergen-induced responses in asthmatic subjects [O] . P.L. Harbinson, D. MacLeod, R. Hawksworth, 1997

机译：新型口服活性选择性PDE4同工酶抑制剂（CDP840）对哮喘受试者中过敏原诱导的反应的影响

Orally active PDE4 inhibitors with therapeutic potential.

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