Identification of a novel antifungal backbone of naphthalimide thiazoles with synergistic potential for chemical and dynamic treatment
Aim: The high incidence and prevalence of fungal infections call for new antifungal drugs. This work was to develop naphthalimide thiazoles as potential antifungal agents. Results & methodology: These compounds showed significant antifungal potency toward some tested fungi. Especially, naphthalimide thiazole 4h with excellent anti-Candida tropicalis efficacy possessed good hemolysis level, low toxicity and no obvious resistance. Deciphering the mechanism showed that 4h interacted with DNA and disrupted the antioxidant defense system of C. tropicalis. Compound 4h also triggered membrane depolarization, leakage of cytoplasmic contents and LDH inhibition. Simultaneously, 4h rendered metabolic inactivation and eradicated the formed biofilms of C. tropicalis. Conclusion: The multifaceted synergistic effect initiated by naphthalimide thiazoles is a reasonable treatment window for prospective development.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2021 |
|---|---|
| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:13 |
|---|---|
| Enthalten in: |
Future medicinal chemistry - 13(2021), 23 vom: 01. Dez., Seite 2047-2067 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Zhang, Peng-Li [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
Antifungal |
|---|
| Anmerkungen: |
Date Completed 10.01.2022 Date Revised 10.01.2022 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.4155/fmc-2021-0162 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM332129632 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM332129632 | ||
| 003 | DE-627 | ||
| 005 | 20231225214950.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2021 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/fmc-2021-0162 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1107.xml |
| 035 | |a (DE-627)NLM332129632 | ||
| 035 | |a (NLM)34672778 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Zhang, Peng-Li |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Identification of a novel antifungal backbone of naphthalimide thiazoles with synergistic potential for chemical and dynamic treatment |
| 264 | 1 | |c 2021 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 10.01.2022 | ||
| 500 | |a Date Revised 10.01.2022 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: The high incidence and prevalence of fungal infections call for new antifungal drugs. This work was to develop naphthalimide thiazoles as potential antifungal agents. Results & methodology: These compounds showed significant antifungal potency toward some tested fungi. Especially, naphthalimide thiazole 4h with excellent anti-Candida tropicalis efficacy possessed good hemolysis level, low toxicity and no obvious resistance. Deciphering the mechanism showed that 4h interacted with DNA and disrupted the antioxidant defense system of C. tropicalis. Compound 4h also triggered membrane depolarization, leakage of cytoplasmic contents and LDH inhibition. Simultaneously, 4h rendered metabolic inactivation and eradicated the formed biofilms of C. tropicalis. Conclusion: The multifaceted synergistic effect initiated by naphthalimide thiazoles is a reasonable treatment window for prospective development | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a antifungal | |
| 650 | 4 | |a naphthalimide | |
| 650 | 4 | |a reactive oxidative species | |
| 650 | 4 | |a thiazole | |
| 650 | 7 | |a Antifungal Agents |2 NLM | |
| 650 | 7 | |a Naphthalimides |2 NLM | |
| 650 | 7 | |a Thiazoles |2 NLM | |
| 700 | 1 | |a Lavanya, Gopala |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Yang |e verfasserin |4 aut | |
| 700 | 1 | |a Fang, Bo |e verfasserin |4 aut | |
| 700 | 1 | |a Zhou, Cheng-He |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Future medicinal chemistry |d 2009 |g 13(2021), 23 vom: 01. Dez., Seite 2047-2067 |w (DE-627)NLM194822109 |x 1756-8927 |7 nnns |
| 773 | 1 | 8 | |g volume:13 |g year:2021 |g number:23 |g day:01 |g month:12 |g pages:2047-2067 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/fmc-2021-0162 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 13 |j 2021 |e 23 |b 01 |c 12 |h 2047-2067 | ||