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Synthesis and antimycobacterial activity of some phthalimide derivatives.

Abstract：

:Structurally modified phthalimide derivatives were prepared through condensation of phthalic and tetrafluorophthalic anhydride with selected sulfonamides with variable yields. All compounds were screened for their antimycobacterium activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) using a micro broth dilution technique. The fluorinated derivatives (compounds 2c, 2d, 2f and 2h) had antimycobacterium activity comparable with classical sulfonamide drugs. The minimum inhibitory concentration (MIC) of compounds 2c, 2d, 2f and 2h was greater than that of isoniazid (MIC<0.02 μg/mL) and in vitro activity was greater than that of pyrazinamide, another first line antimycobacterium drug (MIC 50-100 μg/mL). The new compounds could be considered new lead compounds in the treatment of multi-drug resistant tuberculosis.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Akgün H,Karamelekoğlu I,Berk B,Kurnaz I,Sarıbıyık G,Oktem S,Kocagöz T

doi

10.1016/j.bmc.2012.04.060

subject

Has Abstract

pub_date

2012-07-01 00:00:00

pages

4149-54

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00357-4

journal_volume

20

pub_type

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