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吡唑衍生物作为治疗炎症的选择性COX-2抑制剂的最新进展综述。

Review of the recent advances of pyrazole derivatives as selective COX-2 inhibitors for treating inflammation.

作者信息

Ghoneim Mohammed M, Abdelgawad Mohamed A, Elkanzi Nadia A A, Bakr Rania B

机构信息

Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Ad Diriyah, 13713, Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, 72388, Saudi Arabia.

出版信息

Mol Divers. 2025 Apr;29(2):1789-1820. doi: 10.1007/s11030-024-10906-9. Epub 2024 Jul 16.

Abstract

Pyrazole heterocycle is regarded as an extremely significant agent for the therapy of inflammation. Celecoxib, lonazolac, deracoxib, and phenylbutazone are examples of commercially approved pyrazole drugs with COX-2 inhibitory potential for curing inflammation. There have been recently many reviews for the biological significance of pyrazole derivatives. This review talks about pyrazole derivatives with anti-inflammatory activity and also sheds the light on the recent updates on pyrazole research with an emphasis on some synthetic pathways utilized to construct this privileged scaffold and structure activity relationship that accounts for the anti-inflammatory activity in an attempt to pave the opportunity for medicinal chemists to develop novel anti-inflammatory agents with better COX-2 selectivity.

摘要

吡唑杂环被认为是治疗炎症的极其重要的药物。塞来昔布、氯那唑酸、德拉考昔和保泰松是商业上已批准的具有COX - 2抑制潜力用于治疗炎症的吡唑类药物的例子。最近有许多关于吡唑衍生物生物学意义的综述。本综述讨论了具有抗炎活性的吡唑衍生物,还阐述了吡唑研究的最新进展,重点介绍了用于构建这一特殊骨架的一些合成途径以及解释抗炎活性的构效关系,试图为药物化学家开发具有更好COX - 2选择性的新型抗炎药物创造机会。

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