Author/Authors :
John J.M. Wiener، نويسنده , , Laurent Gomez، نويسنده , , Hariharan Venkatesan، نويسنده , , Alejandro Santill?n Jr.، نويسنده , , Brett D. Allison، نويسنده , , Kimberly L. Schwarz، نويسنده , , Shirin Shinde، نويسنده , , Liu Tang، نويسنده , , Michael D. Hack، نويسنده , , Brian J. Morrow، نويسنده , , S. Timothy Motley، نويسنده , , Raul M. Goldschmidt، نويسنده , , Karen Joy Shaw، نويسنده , , Todd K. Jones، نويسنده , , Cheryl A. Grice، نويسنده ,
Abstract :
We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type II bacterial topoisomerases. Herein are reported SAR investigations of this new series. Several compounds possessing broad-spectrum potency were prepared. Further, these compounds exhibit activity against multidrug-resistant Gram-positive microorganisms equivalent to that against susceptible strains.
Keywords :
Quinolone , gyrase , Topoisomerase , Bacteria , bacterial resistance , SAR , MIC , broad-spectrum , Antibacterial , Escherichia coli , Staphylococcus aureus , Streptococcus pneumoniae , Tetrahydroindazole