A series of 9-sulfonylated/sulfenylated-6-mercaptopurines has been prepared by reaction of 6-mercaptopurine with sulfonyl/sulfenyl halides. These compounds constitute a new class of potent antimycobacterial agents, possessing MIC values against Mycobacterium tuberculosis H37Rv in the range of 0.39-3.39 microg/mL, as well as appreciable activity against Mycobacterium avium. Furthermore, a compound of this small series exhibited good activity (MIC under 1 microg/mL) against several drug resistant strains of M. tuberculosis.
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives / A. Scozzafava;A. Mastrolorenzo;C. T. Supuran. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 11:(2001), pp. 1675-1678.
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
SCOZZAFAVA, ANDREA;SUPURAN, CLAUDIU TRANDAFIR
2001
Abstract
A series of 9-sulfonylated/sulfenylated-6-mercaptopurines has been prepared by reaction of 6-mercaptopurine with sulfonyl/sulfenyl halides. These compounds constitute a new class of potent antimycobacterial agents, possessing MIC values against Mycobacterium tuberculosis H37Rv in the range of 0.39-3.39 microg/mL, as well as appreciable activity against Mycobacterium avium. Furthermore, a compound of this small series exhibited good activity (MIC under 1 microg/mL) against several drug resistant strains of M. tuberculosis.
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