Title of article :
2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis
Author/Authors :
Zhong Li، نويسنده , , Gerardo D. Francisco، نويسنده , , William Hu، نويسنده , , Pornpen Labthavikul، نويسنده , , Peter J. Petersen، نويسنده , , Anatoly Severin، نويسنده , , Guy Singh، نويسنده , , Youjun Yang، نويسنده , , Beth A. Rasmussen، نويسنده , , Yang-I Lin، نويسنده , , Jerauld S. Skotnicki، نويسنده , , Tarek S. Mansour، نويسنده ,
Abstract :
Twenty-five 2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives were synthesized for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good inhibitory activity against Staphylococcus aureus MurB, MurC and MurD enzymes in vitro and antimicrobial activity against gram-positive bacteria including MRSA, VRE and PRSP. However, when they were tested in the presence of 4% bovine serum albumin, the MIC values increased to greater than 128 μg/mL against PRSP. None of the compounds demonstrated activity against gram-negative bacteria at MIC <32 μg/mL.
