含磺酰基哌嗪的拉扎酰胺是治疗青光眼相关症状的有效药物

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2024-09-25 DOI:10.1002/cmdc.202400601

fabrizio carta, Jaydeo T. Kilbile, Suryakant B. Sapkal, Gioele Renzi, Ilaria D’Agostino, Mohamed Boudjelal, Yasinalli Tamboli, Luigi Cutarella, Mattia Mori, Silvia Sgambellone, Serafina Villano, Silvia Marri, Laura Lucarini, Simone Carradori, Claudiu T. Supuran

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引用次数: 0

摘要

通过对 Lasamide 1 与取代的哌嗪进行酰胺化，设计并合成了一系列 2,4-二氯-5-{[4-（苯磺酰基）哌嗪-1-基]羰基}苯磺酰胺。新得到的化合物对人（h）表达的碳酸酐酶（CA；EC 4.2.1.1）II 同工酶具有显著的抑制效力和选择性。在青光眼的体内模型中对所选化合物 7 和 9 进行了研究，结果表明这两种化合物具有相关的性能，其中后者的作用时间可长达 4 小时。本文报告的结果表明，Lasamide 衍生物是一类新的化合物，可用于治疗不受控制的眼压。

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Lasamide Containing Sulfonylpiperazines as Effective Agents for the Management of Glaucoma Associated Symptoms

A series of 2,4-dichloro-5-{[4-(phenylsulfonyl)piperazin-1-yl]carbonyl}benzenesulfonamide were designed and synthesized through amidation of Lasamide 1 with substituted piperazines. The newly obtained compounds demonstrated remarkable inhibition potency and selectivity for the human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) II isoform. Selected compounds 7 and 9 were considered in an in vivo model of glaucoma and showed relevant performances with the latter being able to last the effect up to 4 hours. The results herein reported are in sustainment of Lasamide derivatives as a new class of compounds potentially exploitable for the management of uncontrolled IOP.

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来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.