The antimycobacterial activities of two new S-alkylisothiosemicarbazone derivatives (1i and 1f) against 32 Mycobacterium avium isolates were investigated. The minimum inhibitory concentrations (MICs) were significantly lower than those of... more
The antimycobacterial activities of two new S-alkylisothiosemicarbazone derivatives (1i and 1f) against 32 Mycobacterium avium isolates were investigated. The minimum inhibitory concentrations (MICs) were significantly lower than those of rifampicin and other reference drugs. The two derivatives also showed excellent intracellular activity against M. avium residing in the macrophage-like J774 cells. Interestingly, the combination of subinhibitory concentrations of 1i and rifabutin or rifampicin induced a potent synergistic effect, as determined by the fractional inhibitory concentration indexes (FICIs) ranging between 0.103 and 0.412. Such synergistic effect resulted in a 81-fold and 139-fold reduction of the MICs of rifabutin and rifampicin, respectively. Enhancement of intracellular activity of rifabutin by the S-alkylisothiosemicarbazone derivative 1i was also observed. Results indicate that S-alkylisothiosemicarbazones can be useful in the therapy and prophylaxis of M. avium inf...
Research Interests: Medicinal Chemistry, Medical Microbiology, Biology, Medicine, Cell line, and 13 moreMice, Animals, Anti-Bacterial Agents, Antimicrobial agents, Microbial Sensitivity Tests, Drug Interaction, Rifamycins, Minimum inhibitory concentration, Molecular Structure, Mycobacterium avium, Synergistic effect, Mycobacterium avium complex, and Pharmacology and pharmaceutical sciences
9,10-Anthracenedione derivatives are known to exhibit a quite potent anticancer activity. It has also been reported that these compounds can be effectively employed in both antibacterial and antitrypanosomal therapy. Anthraquinones also... more
9,10-Anthracenedione derivatives are known to exhibit a quite potent anticancer activity. It has also been reported that these compounds can be effectively employed in both antibacterial and antitrypanosomal therapy. Anthraquinones also exhibit some undesirable side effects, like cardiotoxicity. So many interactions seem to demonstrate that 9,10-anthracenediones strongly interact with a number of biological sites. In this paper we wish to report on the synthesis and the pharmaceutical activity of some newly synthesised derivatives containing the anthraquinone pharmacophore.
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ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select... more
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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Research Interests: Engineering, Inorganic Chemistry, Organic Chemistry, Heterocyclic chemistry, Cell Cycle, and 33 moreNanotechnology, Apoptosis, Catalyst, Humans, Mice, Animals, Lignans, Viruses, Anti-inflammatory agents, CHEMICAL SCIENCES, Amino Acids, Molecules, Rats, Edema, Trypanosoma brucei brucei, Agricultural and Food Chemistry, Bioorganic and medicinal Chemistry, Cell Proliferation, Biological activity, Pyrazoles, Benzimidazoles, Quaternary Ammonium Compounds, Salts, Structure activity Relationship, Complex, Cell Survival, Antineoplastic Agents, Lactones, Analgesics, Emodin, Pain Threshold, Antiviral Agents, and Molecular Structure
ABSTRACT Differently substituted isonicotinoylhydrazothiazoles and isonicotinoyl-N4-substituted thiosemi-carbazides have been prepared and characterized by means of elemental analysis, 1H-NMR, 13C-NMR, and Mass spectrometry. All the... more
ABSTRACT Differently substituted isonicotinoylhydrazothiazoles and isonicotinoyl-N4-substituted thiosemi-carbazides have been prepared and characterized by means of elemental analysis, 1H-NMR, 13C-NMR, and Mass spectrometry. All the synthesised compounds have been screened in order to evaluate their antimycobacterial activity in vitro. Some of the new compounds showed activity towards M. tuberculosis H37R and M. Marinum in the millimolar range.
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9,10-Anthracenedione derivatives are known to exhibit a quite potent anticancer activity. It has also been reported that these compounds can be effectively employed in both antibacterial and antitrypanosomal therapy. Anthraquinones also... more
9,10-Anthracenedione derivatives are known to exhibit a quite potent anticancer activity. It has also been reported that these compounds can be effectively employed in both antibacterial and antitrypanosomal therapy. Anthraquinones also exhibit some undesirable side effects, like cardiotoxicity. So many interactions seem to demonstrate that 9,10-anthracenediones strongly interact with a number of biological sites. In this paper we wish to report on the synthesis and the pharmaceutical activity of some newly synthesised derivatives containing the anthraquinone pharmacophore.