醋甲唑胺(Methazolamide) - 药物靶点：CAs_在研适应症：青光眼_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Methazolamide (JAN/USP/INN)、Methenamide、Neptazaneat

+ [6]

靶点

CAs

作用方式

抑制剂

作用机制

CAs抑制剂(碳酸酐酶家族抑制剂)

治疗领域

眼部疾病

在研适应症

青光眼

非在研适应症-

原研机构

Lederle Laboratories

在研机构-

非在研机构

Lederle Laboratories

最高研发阶段批准上市

首次获批日期

美国 (1959-01-26),

青光眼

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C5H8N4O3S2

InChIKeyFLOSMHQXBMRNHR-UHFFFAOYSA-N

CAS号554-57-4

关联

14

项与醋甲唑胺相关的临床试验

ChiCTR2400089203

/ Suspended临床4期IIT

Comparative Study on the Clinical Efficacy of Methazolamide and Acetazolamide in the Prevention of Acute Mountain Sickness

开始日期2024-09-08

申办/合作机构-

NCT05575180

/ Completed临床4期IIT

Effect of Acetazolamide and Methazolamide on Hypoxic Exercise Performance

A single-centered randomized doubled blinded placebo-controlled cross-over trial comparing two the effect of two carbonic anhydrase inhibitors on exercise performance in acute hypoxia. Participants will be young (under 40 years of age), healthy males and females who are regularly physically active.

开始日期2023-08-11

申办/合作机构

The University of Waterloo

[+1]

NCT05498103

/ Active, not recruiting临床4期IIT

Use of Methazolamide to Lower Intraocular Pressure

The purpose of this study is to evaluate the effect of methazolamide, 25 mg or 50 mg tablets once a day for a week than twice a day for a week, on lowering intraocular pressure and the safety of methazolamide.

开始日期2023-02-17

申办/合作机构

University of Colorado Denver

100 项与醋甲唑胺相关的临床结果

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100 项与醋甲唑胺相关的转化医学

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100 项与醋甲唑胺相关的专利（医药）

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828

项与醋甲唑胺相关的文献（医药）

2025-02-07·Polycyclic Aromatic Compounds

Design, Synthesis and In-Vitro Antimicrobial and Cytotoxic Activity Screening of 5-Carboxamide Substituted 3, 4-Dihydropyrimidine-2 (1H) Ones

作者: Soleimani Zar, Fereshteh ; Dilmaghani, Karim A. ; Sarveahrabi, Yasin

This paper describes the synthesis and in vitro biol. evaluation of new compounds designated as and .These compounds were synthesized by the reaction of thiazole derivative or thiadiazole derivative with urea and various aromatic aldehydes in ethanol.The structures of the synthesized compounds were checked by IR,¹H,¹³C NMR, and Mass spectroscopy.The antibacterial and antifungal activities of the compounds were evaluated against Escherichia coli (Gram-neg.), Staphylococcus aureus (Gram-pos.), and Candida albicans (fungus) using agar well diffusion, min. inhibitory concentration (MIC), and min. bactericidal/fungicidal concentration methods.The cytotoxic activities of these compounds against HT-29 and A-549 cancer cell lines were assessed in vitro by the MTT method.Our studies showed compounds and to have the most expressed antibacterial activity against S. aureus, while compounds and were the most potent against E. coli.Compounds and showed the highest antifungal activity against C. albicans, and compound showed the most potent activity against the tested cancer cell lines.

2025-02-01·Journal of Sleep Research

Effects of the low Fowler's sleep position and methazolamide treatment on sleep bruxism: A randomized controlled trial

Article

作者: Zhong, Zhijun ; Yao, Dongyuan ; Ouyang, Qian ; Zhang, Ling ; Liu, Xinting ; Zou, Xueliang ; Luo, Yaxing ; Li, Qi

SummaryIntracranial pressure is one of the determinants of sympathetic activities, and sleep bruxism is associated with increased sympathetic activities. This study aimed to investigate effects of the low Fowler's sleep position and methazolamide treatment on the occurrence of rhythmic masticatory muscle activities/sleep bruxism episodes in patients with sleep bruxism in a randomized controlled trial. Polysomnographic recordings were performed on the patients with sleep bruxism sleeping in the low Fowler's (15°–30°) or supine position (n = 11), and with methazolamide or placebo treatment (100 mg, 3–4 hr before bedtime, P.O., n = 9), and changes in sleep variables and heart rate variance during sleep in the low Fowler's position or with methazolamide treatment were determined. Sleep bruxism index, number of masseter muscle electromyographic bursts per hour of sleep, ratio of rhythmic masticatory muscle activities/sleep bruxism duration to the total sleep duration, index of total limb movements, index of limb movements with rhythmic masticatory muscle activities, and number of sleep bruxism clusters per hour of sleep in the low Fowler's position and after methazolamide intake were significantly smaller (p < 0.05–0.001) than those in the supine position and after placebo intake, respectively. The low‐frequency heart rate variance powers during non‐rapid eye movement sleep stage 2 (N2) in the low Fowler's position and with methazolamide treatment were significantly lower (p < 0.05) than those during sleep in the supine position and with placebo treatment, respectively. In conclusion, sleep in the low Fowler's position and methazolamide treatment were associated with significant decreases in the occurrence of rhythmic masticatory muscle activities/sleep bruxism episodes, which might be due to a reduction in intracranial pressure and sympathetic activities mainly during non‐rapid eye movement sleep stage 2.

2025-02-01·Bioorganic Chemistry

Synthesis, biological evaluation, and in silico studies of phenyl naphthalene-2-sulfonate derived thiosemicarbazones as potential carbonic anhydrase inhibitors

Article

作者: Talib, Rimsha ; Li, Jing ; Aftab, Hina ; Sadeghian, Nastaran ; Tariq, Hafiza Zara ; Şenol, Halil ; Alharthy, Rima D ; Eshal, Javeria ; Akram, Muhammad Safwan ; Taslimi, Parham ; Shafiq, Zahid

A series of novel phenyl naphthalene-2-sulfonate-based thiosemicarbazones (5a-v) were synthesized and evaluated for their inhibitory activity against human carbonic anhydrases I and II (hCA I and hCA II). Compounds 5d and 5p demonstrated the highest inhibitory potency, with IC₅₀ values of 4.32 ± 0.02 nM and 5.24 ± 0.03 nM for hCA I, and 3.89 ± 0.01 nM and 4.72 ± 0.01 nM for hCA II, respectively. Notably, compound 5d exhibited superior potency compared to the reference drug acetazolamide. The structure-activity relationship (SAR) analysis revealed that electron-withdrawing groups, particularly the dichlorophenyl group in 5d and 5p, enhanced inhibitory activity. Molecular docking and molecular dynamics simulations confirmed the high binding affinity of compound 5d, with docking scores of -9.7 kcal/mol for hCA I and -9.5 kcal/mol for hCA II. Stability in MD simulations further supported its potent inhibitory action. ADMET predictions suggested that compounds 5d and 5p have favorable pharmacokinetic profiles. In conclusion, phenyl naphthalene-2-sulfonate-based thiosemicarbazones, especially compound 5d, show strong potential as therapeutic agents targeting hCA I and hCA II.

100 项与醋甲唑胺相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00655	醋甲唑胺	S01EC05	DB00703

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
青光眼	美国	-	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02463357 (CTgov)	临床4期	高原反应	148	Quercetin (Quercetin)	遞衊選糧簾鑰遞壓遞廠(淵醖製壓顧鏇膚鏇衊憲) = 衊衊鹹壓鹹壓壓蓋觸壓鏇遞膚憲鏇鏇廠鑰膚製 (糧網觸簾選願觸憲願夢, 鹹構顧範積簾觸鹹鑰憲 ~ 鬱鏇構繭繭鏇壓蓋製鹽) 更多	-	2021-03-30
				Methazolamide+Nifedipine extended release (Nifedipine+Methazolamide)	遞衊選糧簾鑰遞壓遞廠(淵醖製壓顧鏇膚鏇衊憲) = 鏇築艱構繭憲淵鬱齋遞鏇遞膚憲鏇鏇廠鑰膚製 (糧網觸簾選願觸憲願夢, 蓋膚壓鑰艱構製襯壓齋 ~ 製蓋鏇遞積鏇繭鬱夢廠) 更多
Abstract 2013 (AACR2019)	N/A	胰腺癌	-	Methazolamide + Gemcitabine	糧艱鹽齋夢膚齋衊餘簾(窪襯製夢鹽鑰窪衊繭餘) = anti-angiogenic potential viz. would healing, tube formation and expression of important anti-angiogenic markers like HIF1α, VEGF were profoundly modulated in MZM and combination group 齋齋襯選餘鬱餘顧餘繭 (獵願餘觸艱壓艱鬱艱網 ) 更多	积极	2019-07-01
				Methazolamide
NCT02758470 (Pubmed \| J Appl Physiol (1985))	临床4期	缺氧	13	Acetazolamide	糧鹽醖糧顧顧顧糧構願(艱夢顧窪蓋醖襯觸觸觸) = 網齋醖憲築襯艱範構蓋鏇簾遞憲遞獵壓觸構艱 (鬱壓夢艱網範築鬱範襯 ) 更多	-	2018-09-01
				Methazolamide	糧鹽醖糧顧顧顧糧構願(艱夢顧窪蓋醖襯觸觸觸) = 積淵襯選顧憲襯廠齋餘鏇簾遞憲遞獵壓觸構艱 (鬱壓夢艱網範築鬱範襯 ) 更多
NCT01587027 (CTgov)	临床1期	高原反应	16	Methazolamide+Aminophylline (Sequence A)	醖鏇構艱餘餘簾衊積壓(範夢壓簾鏇鏇艱積襯窪) = 觸鹹淵憲壓願醖憲鹽壓鏇襯鬱夢壓襯餘鹽窪網 (積製齋憲齋選膚餘窪選, 範鬱襯壓鑰衊簾鹹顧齋 ~ 鹹廠網獵網鏇醖築齋衊)	-	2014-06-09
				Methazolamide+Aminophylline (Sequence B)	醖鏇構艱餘餘簾衊積壓(範夢壓簾鏇鏇艱積襯窪) = 遞觸衊鹹遞蓋鹹壓憲鏇鏇襯鬱夢壓襯餘鹽窪網 (積製齋憲齋選膚餘窪選, 醖蓋糧範醖網衊餘願鏇 ~ 獵襯膚鹹願簾齋顧淵壓)
AAO2002	N/A	Stevens-Johnson综合征	-	Methazolamide	(糧遞鹹餘廠襯艱願範壓) = 憲構製襯憲憲獵窪醖簾積簾築餘憲壓積淵膚糧 (蓋願鬱壓顧夢鏇構廠窪 ) 更多	-	2002-10-22