Anti-infectives A∥ rights re served Structure-activity relationships Controls potency, Adds iram Positiye activity NH2>OHSCH3>H ssential for Gyrase Binding . il other gro and Bacterial Tranport No modifi Controls gyrase an less active Bacterial potency 5-100x more active than 5 any other groups F 5 C—OH Controls. Potency, Spectrum. Close to Gyrase fand pharmacokinetics Binding site 5-& 6-membered rings most active. Basic R 7 R2 to R1 or C3 acid are active oral efficacy. Best Gram(+) Potency Controls R Pharmacokinetics. and Anaerobe Activity Controls Potency For Oral Activity Some effect on Pharmacokinetics Best Gram()Potency CF CCbN>COMe>CH For Activity For Best Anaerobe Activity CcCF≥COMe>>CHN 厶 cH1>◇>CH3CH2 Much less active are: CH3 CH3 Ring alkylation CCH3, CCN, CBr, CSR FCH2CH2 improves Gram CNH2, COH, CCH2OH O or N reduce activity activity and Tn P海医药工业研究院 SFPHGRMACEUTCAL NDUSTRYAnti-infectives All rights re served Structure-activity relationships