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用于中性粒细胞主导的炎症性疾病的新型大环内酯类药物的设计。

The design of novel classes of macrolides for neutrophil-dominated inflammatory diseases.

机构信息

Fidelta d.o.o., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia.

出版信息

Future Med Chem. 2014 Apr;6(6):657-74. doi: 10.4155/fmc.14.14.

DOI:10.4155/fmc.14.14
PMID:24895894
Abstract

Neutrophil-dominated inflammatory diseases, like chronic obstructive pulmonary disease, cystic fibrosis, bronchiectasis, bronchiolitis obliteras syndrome and non-eosinophilic asthma, present a significant medical problem lacking adequate therapy. Macrolide antibiotics have been reported to be effective in the treatment of the aforementioned diseases, for reasons unrelated to their antibacterial action. This has resulted in research activities aimed at gaining a better understanding of the immunomodulatory actions of macrolides and the synthesis of various novel anti-inflammatory macrolides without antimicrobial activity. Despite the difficult chemistry and lack of an extensive knowledge for their mechanism of action, several interesting molecules from this class, including potential clinical candidates, are on the horizon.

摘要

中性粒细胞为主的炎症性疾病,如慢性阻塞性肺疾病、囊性纤维化、支气管扩张症、闭塞性细支气管炎综合征和非嗜酸性哮喘,是一个严重的医学问题,缺乏有效的治疗方法。大环内酯类抗生素已被报道在上述疾病的治疗中有效,原因与它们的抗菌作用无关。这导致了旨在更好地了解大环内酯类的免疫调节作用和合成各种新型无抗菌活性的抗炎大环内酯类的研究活动。尽管化学性质复杂,作用机制知之甚少,但该类药物中有几个有趣的分子,包括有潜力的临床候选药物,正在崭露头角。

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1
The design of novel classes of macrolides for neutrophil-dominated inflammatory diseases.用于中性粒细胞主导的炎症性疾病的新型大环内酯类药物的设计。
Future Med Chem. 2014 Apr;6(6):657-74. doi: 10.4155/fmc.14.14.
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Long-term macrolide treatment of chronic inflammatory airway diseases: risks, benefits and future developments.长期大环内酯类药物治疗慢性炎症性气道疾病:风险、获益和未来发展。
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Approaches to the synthesis of immunolides: selective immunomodulatory macrolides for cystic fibrosis.免疫内酯的合成方法:用于囊性纤维化的选择性免疫调节大环内酯类药物
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Inflamm Res. 2017 Jan;66(1):1-12. doi: 10.1007/s00011-016-0988-0. Epub 2016 Sep 28.