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更新于：2025-05-07

Broxyquinoline

溴羟喹啉

更新于：2025-05-07

概要

基本信息

药物类型

小分子化药

别名

靶点

MTHFR

作用方式

调节剂

作用机制

MTHFR调节剂(亚甲基四氢叶酸还原酶调节剂)

治疗领域

泌尿生殖系统疾病

在研适应症

阴道炎

非在研适应症-

原研机构-

在研机构-

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C9H5Br2NO

InChIKeyZDASUJMDVPTNTF-UHFFFAOYSA-N

CAS号521-74-4

关联

100 项与溴羟喹啉相关的临床结果

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100 项与溴羟喹啉相关的转化医学

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100 项与溴羟喹啉相关的专利（医药）

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649

项与溴羟喹啉相关的文献（医药）

2025-05-01·Journal of Inorganic Biochemistry

The antibacterial activity and selectivity of bismuth(III) tris(8-hydroxyquinolinates)

Article

作者: Andrews, Philip C ; Duffin, Rebekah N ; Meagher, Laurence ; Soukup, Charles R M ; Burke, Kirralee J

The series of bismuth(III) tris(8-hydroxyquinolinates); [Bi(Q")₃] (1), [Bi(Q'Cl)₃] (2), [Bi(QCl₂)₃] (3), [Bi(QBr₂)₃] (4), and [Bi(QI₂)₃] (5) (where Q"-H = C₉H₇NO; Q'Cl-H = C₉H₆NOCl, QCl₂-H = C₉H₅NOCl₂; QBr₂-H = C₉H₅NOBr₂; and QI₂-H = C₉H₅NOI₂) were synthesised, fully characterised, and evaluated for their antibacterial activity towards three Gram-positive bacteria (vancomycin-resistant E. faecalis, S. aureus, methicillin-resistant S. aureus), and four Gram-negative bacteria (A. baumannii, P. aeruginosa, K. pneumoniae, and E. coli) and also their cytotoxicity towards mammalian cells. New crystallographic data on 4 indicates it is dimeric in the solid state through 'Bi₂O₂' bridging which is consistent with data previously reported for 5. The five complexes (1-5) all exhibited good but variable antibacterial activity and selectivity. Complexes 2 and 5 showed significant activity towards Gram-positive bacteria with MIC (minimum inhibitory concentration) values ranging from 0.78 μM - 3.13 μM and selectivity indices of 6.2 - ≥16.0. For Gram-negative species, complexes 3 and 4 exhibited highly selective activity towards multi-drug resistant strains of A. baumannii with a range of MIC values 0.39-1.56 μM and selectivity indices of 3.14-7.23 respectively. While some of the 8-hydroxyquinolines themselves show reasonable antibacterial activity this is generally enhanced through complexation to bismuth(III).

2025-05-01·International Immunopharmacology

Broxyquinoline targets NLRP3 to inhibit inflammasome activation and alleviate NLRP3-associated inflammatory diseases

Article

作者: Wang, Tingting ; Tang, Huaiping ; Chen, Peipei ; Zou, Xinxin ; Xu, Yun ; Ji, Sen-Lin ; Gao, Shenghan ; Wang, Yunshu

The NLR family pyrin domain-containing 3 (NLRP3) inflammasome is responsible for various pathogenic and non-pathogenic damage signals and plays a critical role in host defense against pathogens and physiological damage. However, inflammasome activation and its subsequent effects also lead to a variety of inflammatory diseases. In this study, we identified broxyquinoline, an FDA-approved antimicrobial drug, as a effective NLRP3 inflammasome inhibitor. Broxyquinoline suppressed NLRP3 inflammasome-dependent interleukin-1β (IL-1β) release, but did not affect NLRC4 or AIM2 inflammasome activation. Mechanistically, broxyquinoline directly targets Arg165 of NLRP3 protein, thus preventing NEK7-NLRP3 interaction, NLRP3 oligomerization, and ASC speck formation, without affecting the NF-κB pathway. Consequently, broxyquinoline significantly attenuated the progression of monosodium urate (MSU)-induced peritonitis and myelin oligodendrocyte glycoprotein (MOG₃₅_-₅₅)-induced experimental autoimmune encephalomyelitis (EAE) in murine models. In conclusion, we demonstrated that broxyquinoline directly targets the NLRP3 protein to suppress the activation of NLRP3 inflammasome and provide a promising therapeutic agent for NLRP3 inflammasome-associated diseases.

2025-03-01·Journal of the Iranian Chemical Society

Spectrophotometric trace determination of Fe(II) with 5,7-dibromo-8-hydroxyquinoline and investigating the spectral, antimicrobial, anticancer properties and DFT study of iron complexes

作者: Sumit ; Garg, Amita ; Kusum ; Kumar, Jai ; Kumar, Pawan

Abstract: A simple, selective and versatile spectrophotometric technique has been developed for determination of iron in novel complex of iron with 5,7-Dibromo-8-hydroxyquinoline in a basic medium.The green-colored complex was extractable in chloroform within the pH range of 8.95-8.99 with maximum intensity of color in the wavelength range of 429-439 nm.Anal. techniques confirmed the complex stoichiometry of 1:2 [Fe(II)-DBHQ].Several parameters were also calculated like Sandell^′s sensitivity (0.001953 μg cm^-2), molar absorptivity coefficient (2.849 x 10⁴ L mol^-1 cm^-2), standard deviation of reproducibility (± 0.001048/0.205%), detection limit (0.14 μg/mL) and regression coefficient (0.9497).These parametric values showed higher adaptability, cost-effectiveness and higher sensitivity of the proposed method of complex determination as compared to already reported methods.Computational chem. calculations were studied using DFT, and global reactivity descriptors such as electronegativity, softness, hardness, electron affinity, ionization potential and electrophilicity were estimated with HOMO and LUMO energies.Using MEP anal. possible targets for nucleophilic or electrophilic attacks on the chem. structures of the complex were identified.In vitro anticancer and antimicrobial activity of the complex was further determined, and the complex showed antineoplastic as well as antimicrobial potency, hence showed the novel complex compatibility in antimicrobial and anticancer applications like therapeutic agents and metal-based drugs.

100 项与溴羟喹啉相关的药物交易

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