Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application
Fungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like <i>Candida</i>, <i>Cryptococcus</i>, and <i>Sporothrix</i> posing significant challenges due to rising resistance and limited treatment...
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| Format: | Article |
| Language: | English |
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MDPI AG
2025-01-01
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| Series: | Journal of Fungi |
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| Online Access: | https://www.mdpi.com/2309-608X/11/1/69 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Wallace Cordeiro de Morais |
| collection | DOAJ |
| description | Fungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like <i>Candida</i>, <i>Cryptococcus</i>, and <i>Sporothrix</i> 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 <i>Cryptococcus neoformans</i> and <i>Candida auris</i>, 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. |
| format | Article |
| id | doaj-art-e1fa400afdd34d17978cb6ee9a303aa4 |
| institution | Kabale University |
| issn | 2309-608X |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Journal of Fungi |
| spelling | doaj-art-e1fa400afdd34d17978cb6ee9a303aa42025-01-24T13:37:26ZengMDPI AGJournal of Fungi2309-608X2025-01-011116910.3390/jof11010069Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal ApplicationWallace Cordeiro de Morais0Gustavo Henrique Oliveira Costa1Vinícius Leal Pitcella2João Victor Vanolli Protti3Carolina Paula de Souza Moreira4José Eduardo Gonçalves5Susana Johann6Renata Barbosa de Oliveira7Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilServiço de Desenvolvimento Tecnológico Farmacêutico, Diretoria de Pesquisa e Desenvolvimento, Fundação Ezequiel Dias (FUNED), Belo Horizonte 30510-010, MG, BrazilDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilFungal infections have become a growing concern in healthcare, particularly in immunocompromised individuals, with species like <i>Candida</i>, <i>Cryptococcus</i>, and <i>Sporothrix</i> 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 <i>Cryptococcus neoformans</i> and <i>Candida auris</i>, 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.https://www.mdpi.com/2309-608X/11/1/69fungal infectionsthiazolyl hydrazoneantifungal agentsdrug development |
| spellingShingle | 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 Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application Journal of Fungi fungal infections thiazolyl hydrazone antifungal agents drug development |
| title | Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application |
| title_full | Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application |
| title_fullStr | Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application |
| title_full_unstemmed | Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application |
| title_short | Novel 2-Thiazolylhydrazone with Druggable Properties for Antifungal Application |
| title_sort | novel 2 thiazolylhydrazone with druggable properties for antifungal application |
| topic | fungal infections thiazolyl hydrazone antifungal agents drug development |
| url | https://www.mdpi.com/2309-608X/11/1/69 |
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