de Morais Wallace Cordeiro, Costa Gustavo Henrique Oliveira, Pitcella Vinícius Leal, Protti João Victor Vanolli, Moreira Carolina Paula de Souza, Gonçalves José Eduardo, Johann Susana, de Oliveira Renata Barbosa
Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, Brazil.
Centro de Desenvolvimento Analítico Farmacêutico (CEDAFAR), Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, Brazil.
J Fungi (Basel). 2025 Jan 16;11(1):69. doi: 10.3390/jof11010069.
Fungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like , , and 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 and , 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.
真菌感染在医疗保健领域已成为一个日益受到关注的问题,尤其是在免疫功能低下的个体中,由于耐药性上升和治疗选择有限,像[具体菌种1]、[具体菌种2]和[具体菌种3]这样的菌种带来了重大挑战。作为应对措施,正在探索新型抗真菌药物,包括噻唑基腙。本研究聚焦于新型噻唑基腙衍生物RW3的开发。合成RW3是为了改善其水溶性和药代动力学性质。该化合物显示出广谱抗真菌活性,尤其对[具体菌种4]和[具体菌种5]有效,具有最小的刺激潜力和低细胞毒性。RW3表现出良好的溶解性和高肠道通透性,表明有口服给药的潜力。结果表明RW3作为进一步开发用于系统性真菌感染治疗药物的有前景的先导化合物。这些发现强调了优化药物性质以提高疗效和安全性的重要性,为创新抗真菌治疗的开发开辟了道路。