Gyrase inhibitors and uses thereof.

Abstract

The present invention relates to the prepn. of compds.of formula I (W = N, CH, CF; X = CH, CF; Z = O, NH; R1 = Ph, or heteroaryl ring; R2 = H, or C1-3 aliph.; A = 5-6 membered heteroaryl ring) that inhibit bacterial gyrase and/or Topo IV. Thus, 4-bromo-2,6-difluoroaniline was treated with sodium perborate tetrahydrate in acetic acid to give 5-bromo-1,3-difluoro-2-nitro-benzene which was treated with NaH, and pyrazole to yield 1-(5-bromo-3-fluoro-2-nitro-phenyl)-1H-pyrazole. This pyrazole was reduced using ammonia, and coupled with 3-pyridyl-diethyl borane, followed by redn. using 10% palladium on carbon to give the desired II. These compds., and compns. thereof, are useful in treating bacterial infection. [on SciFinder(R)]