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Biomedical subjects

Leonardo Sechi

Publications and source records attributed to Leonardo Sechi.

4 recordsLinked to original sources

Synthesis, anti-mycobacterial, anti-trichomonas and anti-candida in vitro activities of 2-substituted-6,7-difluoro-3-methylquinoxaline 1,4-dioxides.

A new series of 23 6,7-difluoro-3-methyl-2-phenylthio/phenylsulfonyl/phenylsulfinyl/benzylamino/phenylamino-quinoxaline 1,4-dioxides variously substituted in the phenyl moiety, was synthesized and submitted to in vitro evaluation for anti-mycobacterial, anti-trichomonas, anti-candida, anti-mycoplasma and antibacterial activities. In anti-mycobacterial assays, several compounds resulted active (MIC90 = 2.0-4.0 microg/ml) against Mycobacterium tuberculosis H37Rv. Anti-trichomonas screening showed a generally good activity of all compounds (MBC = 0.39-25.0 microg/ml) versus Trichomonas vaginalis, in particular the derivatives 5a,d, 7a, 9 and 11c ranged 0.39-0.78 microg/ml (metronidazole MBC = 12.5 microg/ml). Results of anti-candida assays showed that derivatives 7a, 8a,d and 9 were active against several species of Candida (C. albicans, C. krusei, C. parapsilosis and C. glabrata), having MIC50 between 3.9 and 31.25 microg/ml. The latter compounds were also submitted to anti-mycoplasma assay against Mycoplasma hominis, the results obtained showed that 7a, 8a,d and 9 inhibited the growth of the mycoplasma at the concentration of 0.1 mg/ml. In antibacterial tests only a few compounds showed an MIC50 lower than 62.5 microg/ml against representative strains of Gram-positive and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio alginolyticus and Pseudomonas aeruginosa).

Animals↗

Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity.

Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio-phenylsulphonyl-chloro-quinoxaline 1,4-dioxides belonging to series 3-6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally good activity of 3-methyl-2-phenylthioquinoxaline 1,4-dioxides (3d,e,h-j) against Mycobacterium tuberculosis, and exhibited MIC between 0.39 and 0.78 microg mL(-1) (rifampicin MIC=0.25 microg mL(-1)), whereas in compounds 4d,e, 5a,b,d,e,l and 6b-e,j,l MIC ranged between 1.56 and 6.25 microg mL(-1). Results of the antibacterial and anticandida screening showed that 6e and 6l exhibited MIC=0.4 and 1.9 microg mL(-1), respectively, against Candida krusei (miconazole MIC=0.9 microg mL(-1)), and 4i, 5b,d, 6e, MIC=3.9 microg mL(-1) against Candida glabrata (miconazole MIC=0.4 microg mL(-1)), while compounds 3d,l, 5e,l, and 6b,d,e,l showed MIC=15.6 microg mL(-1) against Vibrio alginolyticus.

Anti-Bacterial Agents↗