ABSTRACT
The aim of the study was to determine the antifungal effects of the essential oil of Thymus broussonetii Boiss (EOT), an endemic plant in Morocco against Candida albicans, Aspergillus fumigatus and the dermatophytes. EOT was extracted by steam distillation. A suspension of up to 500 µL of C. albicans at a concentration of 108 CFU mL⻹ and A. fumigatus at a concentration of 10¹° spores mL⻹ were inhibited by 20 µL of EOT incorporated in tubes containing 4 mL of Sabouraud broth. In Sabouraud-chloramphenicol agar slants containing different concentrations of essential oil, 5 × 104 A. fumigatus spores were inhibited by 6 µL (0.0015 mL mL⻹) of the EOT. It has shown good anti-C. albicans and anti-A. fumigatus activity. All the dermatophytes tested were inhibited by 3 µL (0.00075 mL mL⻹) of EOT; the latter has the potential to be a good alternative to the conventional antifungal drugs which are usually expensive and with high toxicity.
Subject(s)
Antifungal Agents/chemistry , Oils, Volatile/chemistry , Thymus Plant/chemistry , Antifungal Agents/pharmacology , Arthrodermataceae/drug effects , Aspergillus fumigatus/drug effects , Candida albicans/drug effects , Oils, Volatile/pharmacologyABSTRACT
New homo and heterodimers of ddI, d4T and AZT with (5-5) thiolcarbonate-carbamate linkages have been prepared with the aim of testing them against wild type and NNRTI resistant HIV mutants. The prepared dimers showed a low activity in comparison to the parent drug.
Subject(s)
Anti-HIV Agents/pharmacology , Antiviral Agents/chemistry , Carbamates/chemistry , Didanosine/chemistry , HIV/metabolism , Stavudine/chemistry , Sulfhydryl Compounds/chemistry , Zidovudine/chemistry , Antiviral Agents/pharmacology , Dimerization , HIV/genetics , HIV Infections/drug therapy , Models, Chemical , Molecular Conformation , MutationABSTRACT
Several D-ribonucleosides are prepared from 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranoside and trimethylsilylated nucleobases under mild conditions by using natural phosphate doped with KI as catalyst.
Subject(s)
Molecular Biology/methods , Phosphates/chemistry , Alkylation , Catalysis , Chromatography , Glycosides/chemistry , Glycosylation , Hydrocarbons/chemistry , Indicators and Reagents/chemistry , Methane/analogs & derivatives , Methane/chemistry , Models, Chemical , Nucleosides/chemistry , Potassium Iodide/chemistryABSTRACT
Homo- and heterodimers of AZT and d4T, possessing carbonate and carbamate linkers, have been synthesized with the aim to enhance the antiviral activity of their components. Homo- and heterodimer carbamates showed weak anti-HIV activity. On the other hand, dinucleoside carbonates showed marked antiviral activity.
Subject(s)
Anti-HIV Agents/chemical synthesis , Fungal Proteins/chemistry , Lipase/chemistry , Stavudine/chemical synthesis , Zidovudine/chemical synthesis , Anti-HIV Agents/pharmacology , Cell Line , Dimerization , HIV Infections/drug therapy , HIV Infections/virology , HIV-1/drug effects , HIV-2/drug effects , Humans , Stavudine/pharmacology , Virus Replication/drug effects , Zidovudine/pharmacologyABSTRACT
Doped natural phosphate is used as acidic or basic catalyst in nucleoside and acyclonucleoside synthesis. Some examples are given.
Subject(s)
Nucleosides/chemical synthesis , Phosphates/chemistry , Biological Factors , Catalysis , Kinetics , Mining , Morocco , StereoisomerismABSTRACT
A series of new homo and heterodimers of ddI has been synthesized. A glutarate diester spacer was used to covalently couple ddI onto ddI, AZT or d4T.
Subject(s)
Didanosine/analogs & derivatives , Didanosine/chemistry , Anti-HIV Agents/chemistry , Didanosine/chemical synthesis , Dimerization , Esters , Indicators and Reagents , Molecular Conformation , Stavudine/chemistry , Zidovudine/chemistryABSTRACT
Potassium fluoride doped natural phosphate, inexpensive and environmentally friendly catalyst, is shown to be an efficient basic catalyst for the N1/N9 alkylation of different nucleobases as synthons for PNAs.
Subject(s)
Peptide Nucleic Acids/chemical synthesis , Alkylation , Catalysis , Fluorides/chemistry , Heterocyclic Compounds/chemistry , Magnetic Resonance Spectroscopy , Models, Chemical , Phosphates/chemistry , Potassium Compounds/chemistryABSTRACT
The synthesis of new dinucleosides of AZT and D4T is described.
Subject(s)
Dideoxynucleosides/chemical synthesis , Stavudine/analogs & derivatives , Zidovudine/analogs & derivatives , Anti-HIV Agents/chemical synthesis , Stavudine/chemical synthesis , Zidovudine/chemical synthesisABSTRACT
The synthesis of 1,2,3-triazole acyclonucleosides 7a-h via 1,3-dipolar cycloaddition of N-9/N-1-propargylpurine/pyrimidine 2a-h with azido-pseudo-sugar 4 is described and none of them had anti-HIV activity.
Subject(s)
Anti-HIV Agents/chemical synthesis , Anti-HIV Agents/pharmacology , Nucleosides/chemistry , Nucleosides/pharmacology , Triazoles/chemistry , Biochemistry/methods , HIV-1/drug effects , HIV-2/drug effects , Microbial Sensitivity Tests , Nucleosides/chemical synthesis , Structure-Activity RelationshipABSTRACT
Alkenyl acyclonucleosides derivatives of 5-halogenouracil have been synthesized via Michael addition reaction. These compounds were treated by allylbromide, propargylbromide or ethylbromoacetate to give the corresponding N-1,N-3-disubstituted 5-halogenouracil.