Details

Autor(en) / Beteiligte

• Ali, Mohamed Ashraf
• Shaharyar, Mohammad

Titel

Discovery of novel phenoxyacetic acid derivatives as antimycobacterial agents

Ist Teil von

• Bioorganic & medicinal chemistry, 2007-03, Vol.15 (5), p.1896-1902

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2007

Link zum Volltext

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• A series of 2-{4-[1-amino (thioxo) methyl-5-(substituted phenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid and 2-{4-[1-carbamoyl-5-(substituted phenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid were synthesized and the in vitro activity of the synthesized compounds against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) was studied. Among the synthesized compounds, compound ( 3f) 2{-[4-(1-carbamoyl-5-(chloro phenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy} acetic acid was found to be the mostf active against M. tuberculosis H37Rv (MTB) and INH resistant M. tuberculosis (INHR-MTB) with minimum inhibitory concentration of 0.06 μg/ml. A series of 2-{4-[1-amino (thioxo) methyl-5-(substituted phenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid and 2-{4-[1-carbamoyl-5-(substituted phenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid were synthesized and the in vitro activity of the synthesized compounds against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) was studied. Among the synthesized compounds, compound ( 3f) 2{-[4-(1-carbamoyl-5-(chlorophenyl)-4,5-dihydro-1 H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid was found to be the most active against M. tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) with minimum inhibitory concentration of 0.06 μg/ml.