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Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines

Tonelli, Michele and Novelli, Federica and Tasso, Bruno and Sparatore, Anna and Boido, Vito and Sparatore, Fabio and Cannas, Sara and Molicotti, Paola and Zanetti, Stefania Anna Lucia and Parapini, Silvia and Loddo, Roberta (2014) Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines. Bioorganic & Medicinal Chemistry, Vol. 22 (24), p. 6837-6845. ISSN 0968-0896. eISSN 1464-3391. Article.

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DOI: 10.1016/j.bmc.2014.10.035

Abstract

Novel riminophenazine derivatives, characterized by the presence of the basic and cumbersome quinolizidinylalkyl and pyrrolizidinylethyl moieties, have been synthesized and tested (Rema test) against Mycobacterium tuberculosis H37Rv and H37Ra, and six clinical isolates of Mycobacterium avium and Mycobacterium tuberculosis. Most compounds exhibited potent activity against the tested strains, resulting more active than clofazimine, isoniazid and ethambutol.
The best compounds (4, 5, 12 and 13) exhibited a MIC in the range 0.82–0.86 μM against all strains of Mycobacterium tuberculosis and, with the exception of 4 a MIC around 3.3 μM versus M. avium. The corresponding values for clofazimine (CFM) were 1.06 and 4.23 μM, respectively. Cytotoxicity was evaluated against three cell lines and compound 4 displayed a selectivity index (SI) versus the human cell line MT-4 comparable with that of CFM (SI = 5.23 vs 6.4). Toxicity against mammalian Vero 76 cell line was quite lower with SI = 79.

Item Type:Article
ID Code:10656
Status:Published
Refereed:Yes
Uncontrolled Keywords:Quinolizidinyl- and pyrrolizidinylalkyliminophenazine derivatives, Mycobacterium tuberculosis, Mycobacterium avium Clinical isolates of Mycobacterium tuberculosis, antitubercular activity
Subjects:Area 06 - Scienze mediche > MED/07 Microbiologia e microbiologia clinica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Scienze Biomediche
Publisher:Elsevier
ISSN:0968-0896
eISSN:1464-3391
Deposited On:21 Jan 2015 09:24

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