New Antifungal Agents with Azole Moieties
Fungal conditions affect a multitude of people worldwide, leading to increased hospitalization and mortality rates, and the need for novel antifungals is emerging with the rise of resistance and immunocompromised patients. Continuous use of azole drugs, which act by inhibiting the fungal CYP51, invo...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1424-8247/15/11/1427 |
| _version_ | 1797464247965319168 |
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| author | Melissa Martins Teixeira Diogo Teixeira Carvalho Emília Sousa Eugénia Pinto |
| author_facet | Melissa Martins Teixeira Diogo Teixeira Carvalho Emília Sousa Eugénia Pinto |
| author_sort | Melissa Martins Teixeira |
| collection | DOAJ |
| description | Fungal conditions affect a multitude of people worldwide, leading to increased hospitalization and mortality rates, and the need for novel antifungals is emerging with the rise of resistance and immunocompromised patients. Continuous use of azole drugs, which act by inhibiting the fungal CYP51, involved in the synthesis of ergosterol, essential to the fungal cell membrane, has enhanced the resistance and tolerance of some fungal strains to treatment, thereby limiting the arsenal of available drugs. The goal of this review is to gather literature information on new promising azole developments in clinical trials, with in vitro and in vivo results against fungal strains, and complementary assays, such as toxicity, susceptibility assays, docking studies, among others. Several molecules are reviewed as novel azole structures in clinical trials and with recent/imminent approvals, as well as other innovative molecules with promising antifungal activity. Structure–activity relationship (SAR) studies are displayed whenever possible. The azole moiety is brought over as a privileged structure, with multiple different compounds emerging with distinct pharmacophores and SAR. Particularly, 1,2,3-triazole natural product conjugates emerged in the last years, presenting promising antifungal activity and a broad spectrum against various fungi. |
| first_indexed | 2024-03-09T18:04:52Z |
| format | Article |
| id | doaj.art-ca0b41aaeb4f4f31aab48c6d8163ee25 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T18:04:52Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-ca0b41aaeb4f4f31aab48c6d8163ee252023-11-24T09:35:34ZengMDPI AGPharmaceuticals1424-82472022-11-011511142710.3390/ph15111427New Antifungal Agents with Azole MoietiesMelissa Martins Teixeira0Diogo Teixeira Carvalho1Emília Sousa2Eugénia Pinto3Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalLaboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalLaboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalLaboratory of Microbiology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalFungal conditions affect a multitude of people worldwide, leading to increased hospitalization and mortality rates, and the need for novel antifungals is emerging with the rise of resistance and immunocompromised patients. Continuous use of azole drugs, which act by inhibiting the fungal CYP51, involved in the synthesis of ergosterol, essential to the fungal cell membrane, has enhanced the resistance and tolerance of some fungal strains to treatment, thereby limiting the arsenal of available drugs. The goal of this review is to gather literature information on new promising azole developments in clinical trials, with in vitro and in vivo results against fungal strains, and complementary assays, such as toxicity, susceptibility assays, docking studies, among others. Several molecules are reviewed as novel azole structures in clinical trials and with recent/imminent approvals, as well as other innovative molecules with promising antifungal activity. Structure–activity relationship (SAR) studies are displayed whenever possible. The azole moiety is brought over as a privileged structure, with multiple different compounds emerging with distinct pharmacophores and SAR. Particularly, 1,2,3-triazole natural product conjugates emerged in the last years, presenting promising antifungal activity and a broad spectrum against various fungi.https://www.mdpi.com/1424-8247/15/11/1427antifungal drugsazolesnew developments |
| spellingShingle | Melissa Martins Teixeira Diogo Teixeira Carvalho Emília Sousa Eugénia Pinto New Antifungal Agents with Azole Moieties Pharmaceuticals antifungal drugs azoles new developments |
| title | New Antifungal Agents with Azole Moieties |
| title_full | New Antifungal Agents with Azole Moieties |
| title_fullStr | New Antifungal Agents with Azole Moieties |
| title_full_unstemmed | New Antifungal Agents with Azole Moieties |
| title_short | New Antifungal Agents with Azole Moieties |
| title_sort | new antifungal agents with azole moieties |
| topic | antifungal drugs azoles new developments |
| url | https://www.mdpi.com/1424-8247/15/11/1427 |
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