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N-alkylated 2,3,3-trimethylindolenines and 2-methylbenzothiazoles. Potential lead compounds in the fight against Saccharomyces cerevisiae infections.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2013 Jun; Vol. 64, pp. 222-7. Date of Electronic Publication: 2013 Apr 06. - Publication Year :
- 2013
-
Abstract
- The synthesis of a variety of N-alkylated 2,3,3-trimethylindolenines and 2-methylbenzothiazoles is reported herein. Their potential as antifungal agents is evaluated by preliminary screening against Saccharomyces cerevisiae (S. cerevisiae), Schizosaccharomyces pombe (S. pombe), and Candida albicans (C. albicans). Statistical analyses illustrate a strong relationship between chain length and growth inhibition for S. cerevisiae and S. pombe (p < 0.0001 in every case). Of particular interest is the activity of both sets of compounds against S. cerevisiae, as this is emerging as an opportunistic pathogen, especially in immunosuppressed and immunocompromised patients. Bioassays were set up to compare the efficacy of our range of N-alkylated compounds against classic antifungal agents; Amphotericin B and Thiabendazole.<br /> (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antifungal Agents chemical synthesis
Antifungal Agents chemistry
Benzothiazoles chemical synthesis
Benzothiazoles chemistry
Candida albicans growth & development
Dose-Response Relationship, Drug
Indoles chemical synthesis
Indoles chemistry
Microbial Sensitivity Tests
Molecular Structure
Saccharomyces cerevisiae growth & development
Schizosaccharomyces growth & development
Structure-Activity Relationship
Antifungal Agents pharmacology
Benzothiazoles pharmacology
Candida albicans drug effects
Indoles pharmacology
Saccharomyces cerevisiae drug effects
Schizosaccharomyces drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 64
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23644205
- Full Text :
- https://doi.org/10.1016/j.ejmech.2013.03.031