Based on some homodrimane carboxylic acids and their acyl chlorides, a series of fourteen 2-homodrimenyl-1,3-benzothiazoles, -homodrimenoyl-2-amino-1,3-benzothiazoles, 4'-methyl-homodrimenoyl anilides and 4'-methyl-homodrimenthioyl anilides were synthesized and their biological activities were evaluated on five species of fungi (, , , , and ) and two strains of bacteria ( sp. and ). The synthesis involved the decarboxylative cyclization, condensation and thionation of the said acids, anhydrides or their derivatives with 2-aminothiophenol, 2-aminobenzothiazole, -toluidine and Lawesson's reagent. As a result, together with the desired compounds, some unexpected products , , and were obtained, and the structures and mechanisms for their formation have been proposed. Compounds , , and showed higher antifungal and antibacterial activity compared to the standards caspofungin (MIC = 1.5 μg/mL) and kanamycin (MIC = 3.0 μg/mL), while compound had comparable activities. In addition, compounds , , and showed selective antifungal activity at MIC = 2.0, 0.25, and 1.0 μg/mL, respectively.
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http://dx.doi.org/10.3390/molecules27165082 | DOI Listing |
Biomed Res Int
August 2022
Laboratory of Natural Substances, Pharmacology, Environment, Modeling, Health & Quality of Life (SNAMOPEQ), Polydisciplinary Faculty of Taza (FPT), Sidi Mohamed Ben Abdellah University (USMBA) of Fez, B.P.: 1223 Taza-Gare, Taza, Morocco.
Introduction: The present study is carried out for the first time on L. var. argentea Andre from the region of Taza using an ethnopharmacological survey, an experimental study of the mineralogical and chemical compositions, and evaluations of the antioxidant and antibacterial activities.
View Article and Find Full Text PDFFront Microbiol
July 2022
Department of Dermatology, Jingzhou Hospital, Yangtze University, Candidate Branch of National Clinical Research Center for Skin and Immune Diseases, Jingzhou, China.
Invasive candidiasis is the primary reason for the increased cases of mortality in a medical environment. The resistance spectra of species to antifungal drugs have gradually expanded. Particularly, the resistance spectra of are the most prominent.
View Article and Find Full Text PDFEur J Med Chem
September 2018
Univ. Grenoble Alpes, CNRS, Département de Pharmacochimie Moléculaire, 38000, Grenoble, France. Electronic address:
Amphiphilic aminoglycosides (AAGs) constitute a new class of antibacterial compounds targeting the bacterial membranes. We have identified the 3',6-dinonyl neamine 9 as a broad spectrum antibacterial AAG. Here, we report on the synthesis, antibacterial activity and eukaryotic cytotoxicity of new 3',6-dialkyl neamines designed in order to finely delineate the structure-activity relationships relating their activity to a lipophilicity window.
View Article and Find Full Text PDFClin Microbiol Infect
January 2013
Division of Hygiene and Medical Microbiology, Innsbruck Medical University.
Aspergillus terreus (A. terreus) is of serious concern because of a high propensity to dissemination and in vitro and in vivo resistance to Amphotericin B (AmB). The underlying molecular mechanism of AmB is not known yet and here we want to explore whether fungal heat shock protein 90 (HSP90) is involved in polyene resistance in A.
View Article and Find Full Text PDFRes Microbiol
December 2009
Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11010 Belgrade, Serbia.
Little is known about the diversity and distribution of resistance determinants in human commensal bacteria. The aim of this study was to determine the molecular mechanism responsible for high-level erythromycin resistance among five human vaginal Lactobacillus rhamnosus isolates. PCR screening for the presence of ermA, ermB and ermC methylase genes revealed no determinants responsible for detected erythromycin resistance.
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