PubMed Health⌕ Search

Biomedical subjects

Leonardo Sechi

Publications and source records attributed to Leonardo Sechi.

5 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↗

The infectivity of sarcoid clinical material and its bacterial content inoculated in CBA mice.

BACKGROUND: Sarcoidosis is a multisystemic disorder that is currently viewed as the consequence of chronic immunological response associating genetic susceptibility and specific environmental or transmissible agents. Relevant evidence, although conflicting, justifies a concern about the involvement of specific pathogens to disease causation. In this study we assessed the infectivity of sarcoid clinical material, and of the pathogens found in it, to normal CBA mice used as a model of an immuno-competent host. MATERIALS AND METHODS: One hundred and eleven mice were inoculated into their footpads with fresh, filtered, and autoclaved, sputum and bronchoalveolar lavage homogenates, collected from patients with sarcoidosis, and with the mycobacterial and propionibacterial pathogens isolated from this material. RESULTS: The total number of positive reactors of the animals that received raw clinical material and the pathogens it contained was statistically significant compared to those of the control groups. However, the number of affected mice per group was in most cases less than 50% and inflammation was almost always mild and local. CONCLUSION: Based on the evidence provided by inoculation of normal CBA mice, some of the material under study, although of mild potency, can be infectious to an immuno-competent host.

Animals↗