Screening and Synthesis of Tetrazole Derivatives that Inhibit the Growth of Cryptococcus Species
© 2023 The Authors. ChemMedChem published by Wiley-VCH GmbH..
Cryptococcosis has become a major health problem worldwide and caused morbidity and mortality in immunocompromised patients, especially those infected with human immunodeficiency virus (HIV). Despite the global distribution of cryptococcosis, the number and types of the available antifungals are limited, and the treatment outcomes in HIV patients are generally poor. In this study, we screened a compound library and identified one tetrazole derivative as an efficient inhibitor of Cryptococcus neoformans and Cryptococcus gattii. We further designed and synthesized a series of tetrazole derivatives and determined their structure-activity relationship, demonstrating that tetrazole backbone-containing compounds could be developed as novel antifungal drugs with distinct mechanisms against Cryptococcus spp. Our findings provide a starting point for novel target identification and structural optimization to develop a distinct class of therapeutics for patients with cryptococcosis.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:18 |
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| Enthalten in: |
ChemMedChem - 18(2023), 18 vom: 15. Sept., Seite e202300157 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Nakada, Nana [VerfasserIn] |
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| Links: |
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| Themen: |
Antifungal Agents |
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| Anmerkungen: |
Date Completed 26.09.2023 Date Revised 26.09.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1002/cmdc.202300157 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM359288065 |
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| 520 | |a © 2023 The Authors. ChemMedChem published by Wiley-VCH GmbH. | ||
| 520 | |a Cryptococcosis has become a major health problem worldwide and caused morbidity and mortality in immunocompromised patients, especially those infected with human immunodeficiency virus (HIV). Despite the global distribution of cryptococcosis, the number and types of the available antifungals are limited, and the treatment outcomes in HIV patients are generally poor. In this study, we screened a compound library and identified one tetrazole derivative as an efficient inhibitor of Cryptococcus neoformans and Cryptococcus gattii. We further designed and synthesized a series of tetrazole derivatives and determined their structure-activity relationship, demonstrating that tetrazole backbone-containing compounds could be developed as novel antifungal drugs with distinct mechanisms against Cryptococcus spp. Our findings provide a starting point for novel target identification and structural optimization to develop a distinct class of therapeutics for patients with cryptococcosis | ||
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| 700 | 1 | |a Mizuta, Satoshi |e verfasserin |4 aut | |
| 700 | 1 | |a Hirayama, Tatsuro |e verfasserin |4 aut | |
| 700 | 1 | |a Nakamichi, Seiko |e verfasserin |4 aut | |
| 700 | 1 | |a Takeda, Kohsuke |e verfasserin |4 aut | |
| 700 | 1 | |a Mukae, Hiroshi |e verfasserin |4 aut | |
| 700 | 1 | |a Kohno, Shigeru |e verfasserin |4 aut | |
| 700 | 1 | |a Tanaka, Yoshimasa |e verfasserin |4 aut | |
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