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Synthesis and antimycobacterial evaluation of pyrazinamide derivatives with benzylamino substitution.

Abstract：

:A series of 19 new compounds related to pyrazinamide were synthesized, characterized with analytical data and screened for in vitro whole cell antimycobacterial activity against Mycobacterium tuberculosis H37Rv, Mycobacterium kansasii and two types of Mycobacterium avium. The series consisted of 3-(benzylamino)-5-cyanopyrazine-2-carboxamides and 3-(benzylamino)pyrazine-2,5-dicarbonitriles with various substituents on the phenyl ring. RP-HPLC method was used to determine the lipophilicity of the prepared compounds. Nine compounds exerted similar or better activity against Mycobacterium tuberculosis compared to pyrazinamide (MIC=6.25-12.5 μg/mL). 3-(Benzylamino)pyrazine-2,5-dicarbonitrile inhibited all of the tested mycobacterial strains with MIC within the range 12.5-25 μg/mL. Although not the most active, 4-NH(2) substituted compounds possessed the lowest in vitro cytotoxicity (hepatotoxicity), leading to selectivity index SI=5.5 and SI >21.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zitko J,Paterová P,Kubíček V,Mandíková J,Trejtnar F,Kuneš J,Doležal M

doi

10.1016/j.bmcl.2012.11.052

subject

Has Abstract

pub_date

2013-01-15 00:00:00

pages

476-9

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01504-1

journal_volume

23

pub_type

杂志文章

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