Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application.

IF 4.2 2区 生物学 Q2 MICROBIOLOGY Journal of Fungi Pub Date : 2025-01-16 DOI:10.3390/jof11010069
Wallace Cordeiro de Morais, Gustavo Henrique Oliveira Costa, Vinícius Leal Pitcella, João Victor Vanolli Protti, Carolina Paula de Souza Moreira, José Eduardo Gonçalves, Susana Johann, Renata Barbosa de Oliveira
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Abstract

Fungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like Candida, Cryptococcus, and Sporothrix posing significant challenges due to rising resistance and limited treatment options. In response, novel antifungal agents are being explored, including thiazolyl hydrazones. This study focuses on the development of a novel thiazolylhydrazone derivative, RW3. RW3 was synthesized to improve its water solubility and pharmacokinetic properties. The compound demonstrated a broad antifungal spectrum, particularly effective against Cryptococcus neoformans and Candida auris, with minimal irritant potential and low cytotoxicity. RW3 showed favorable solubility and high intestinal permeability, indicating potential for oral administration. The results suggest RW3 as a promising lead for further development as a therapeutic agent for systemic fungal infections. These findings underscore the importance of optimizing drug properties to enhance efficacy and safety profiles, opening the path for the development of innovative antifungal treatments.

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新型抗真菌药物性质的2-噻唑基腙。
真菌感染已成为医疗保健领域日益关注的问题,特别是在免疫功能低下的个体中,念珠菌、隐球菌和孢子菌等物种由于耐药性上升和治疗方案有限而构成重大挑战。因此,新的抗真菌药物正在被探索,包括噻唑酰腙。本研究的重点是开发一种新的噻唑基腙衍生物RW3。合成RW3以改善其水溶性和药动学性质。该化合物具有广泛的抗真菌谱,特别是对新型隐球菌和耳念珠菌有效,具有最小的刺激潜力和低细胞毒性。RW3具有良好的溶解度和高肠通透性,具有口服给药的潜力。结果表明,RW3作为一种系统性真菌感染的治疗药物,有进一步发展的希望。这些发现强调了优化药物特性以提高疗效和安全性的重要性,为开发创新的抗真菌治疗开辟了道路。
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来源期刊
Journal of Fungi
Journal of Fungi Medicine-Microbiology (medical)
CiteScore
6.70
自引率
14.90%
发文量
1151
审稿时长
11 weeks
期刊介绍: Journal of Fungi (ISSN 2309-608X) is an international, peer-reviewed scientific open access journal that provides an advanced forum for studies related to pathogenic fungi, fungal biology, and all other aspects of fungal research. The journal publishes reviews, regular research papers, and communications in quarterly issues. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible. Therefore, there is no restriction on paper length. Full experimental details must be provided so that the results can be reproduced.
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