首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Pyrazoles and pyrazolines as neural and inducible nitric oxide synthase (nNOS and iNOS) potential inhibitors (III).

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Pyrazoles and pyrazolines as neural and inducible nitric oxide synthase (nNOS and iNOS) potential inhibitors (III).

机译：吡唑和吡唑啉作为神经和诱导型一氧化氮合酶（nNOS和iNOS）的潜在抑制剂（III）。

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We have previously described a series of 4,5-dihydro-1H-pyrazole as moderately potent nNOS inhibitors. As a follow up of these studies, we report here the preparation and the preliminary evaluation of a series of 1-alkyl-3-benzoyl-4,5-dihydro-1H-pyrazole and 1-alkyl-3-benzoyl-1H-pyrazole as potential inhibitors of both neuronal and inducible nitric oxide synthases (nNOS and iNOS). None of the reported compounds exhibited significant iNOS or nNOS inhibition, although the 1-benzyl-3-(2-amino-5-chlorobenzoyl)-1H-pyrazole-5-carboxylic acid ethyl ester derivative (10l), which shows an inhibition of 50% versus iNOS at a 1mM final concentration and no activity against nNOS, is potentially amenable of further optimization. The reasons for the inactivity of the reported series are discussed on the basis of docking studies.

机译：我们之前已经描述了一系列4,5-二氢-1H-吡唑作为中度有效的nNOS抑制剂。作为这些研究的后续，我们在这里报告一系列1-烷基-3-苯甲酰基-4,5-二氢-1H-吡唑和1-烷基-3-苯甲酰基-1H-吡唑的制备和初步评估作为神经元和诱导型一氧化氮合酶（nNOS和iNOS）的潜在抑制剂。尽管1-苄基-3-（2-氨基-5-氯苯甲酰基）-1H-吡唑-5-羧酸乙酯衍生物（10l）对iNOS或nNOS的抑制作用均不明显，但均未显示出对iNOS或nNOS的抑制作用。最终浓度为1mM时，相对于iNOS的50％，并且没有针对nNOS的活性，可能需要进一步优化。在对接研究的基础上讨论了报告的系列不活跃的原因。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第11期|共13页
作者
Carrion MD; Lopez-Cara LC; Camacho ME; Tapias V; Escames G; Acuna-Castroviejo D; Espinosa A; Gallo MA; Entrena A;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
inhibitors; pyrazole; inducible nitric oxide synthase; neural; Pyrazoles; 吡唑类;

机译：抑制剂;吡唑;诱导型一氧化氮合酶;神经;吡唑类;吡唑类;

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1. Pyrazoles and pyrazolines as neural and inducible nitric oxide synthase (nNOS and iNOS) potential inhibitors (III). [J] . Carrion MD, Lopez-Cara LC, Camacho ME, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2008,第11期

机译：吡唑和吡唑啉作为神经和诱导型一氧化氮合酶（nNOS和iNOS）的潜在抑制剂（III）。
2. Concentrations of inducible nitric oxide synthase (iNOS) and neuronal nitric oxide synthase (nNOS) in cerebrospinal fluid of patients with severe head injuries [J] . Uzan M, Tanriover N, Topal Sarikaya A, Neurosurgery quarterly. . 2003,第2期

机译：重型颅脑损伤患者脑脊液中诱导型一氧化氮合酶（iNOS）和神经元一氧化氮合酶（nNOS）的浓度
3. Discovery of Inducible Nitric Oxide Synthase (iNOS) Inhibitor Development Candidate KD7332, Part 1: Identification of a Novel, Potent, and Selective Series of Quinolinone iNOS Dimerization Inhibitors that are Orally Active in Rodent Pain Models [J] . Bonnefous C, Payne JE, Roppe J, Journal of Medicinal Chemistry . 2009,第9期

机译：诱导型一氧化氮合酶（iNOS）抑制剂开发候选者KD7332的发现，第1部分：鉴定在啮齿动物疼痛模型中具有口服活性的新型，有效和选择性系列的喹啉酮iNOS二聚抑制剂
4. Inducible Nitric Oxide Synthase (iNOS) Expression in Cirrhotic Patients with Hepatopulmonary Syndrome [C] . Lifang Sun, Bingquan Zhang, Na Zhang, International conference on environmental biotechnology and materials engineering;EBME 2011 . 2011

机译：肝硬化综合征肝硬化患者中诱导型一氧化氮合酶（iNOS）的表达
5. Development of an indirect enzyme-linked immunosorbent assay for the quantification of inducible nitric oxide synthase protein (iNOS). [D] . Heaton, Phillip R. 2005

机译：间接酶联免疫吸附测定技术的发展，用于定量诱导型一氧化氮合酶蛋白（iNOS）。
6. The return of the Scarlet Pimpernel: cobalamin in inflammation II — cobalamins can both selectively promote all three nitric oxide synthases (NOS) particularly iNOS and eNOS and as needed selectively inhibit iNOS and nNOS [O] . Carmen Wheatley -1

机译：猩红皮鞭的返回：炎症II中的钴胺素-钴胺素既可以选择性地促进所有三种一氧化氮合酶（NOS）特别是iNOS和eNOS又可以根据需要选择性地抑制iNOS和nNOS。
7. Increased expression of constitutive nitric oxide synthase III, but not inducible nitric oxide synthase II, in human heart failure 11During publication process the following related paper has been published by Vejlstrup NG, Bouloumie A, Boesgaard S, Andersen CB, Nielsen-Kudsk JE, Mortensen SA, Kent JD, Harrison DG, Busse R, Alsershvile J. Inducible nitric oxide synthase (iNOS) in the human heart: Expression and localization in congestive heart failure. J Mol Cell Cardiol 1998;30:1215–23. [O] . Stein Birgitt, Eschenhagen Thomas, Rüdiger Jochen, 1998

机译：在人心力衰竭中，组成型一氧化氮合酶III的表达增加，但诱导型一氧化氮合酶II的表达没有增加11 SA，肯特JD，哈里森DG，Busse R，AlsershvileJ。人心中的诱导型一氧化氮合酶（iNOS）：充血性心力衰竭的表达和定位。 J Mol Cell Cardiol 1998； 30：1215-23。

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