Chiral DNA Gyrase Inhibitors. 3. Probing the Chiral Preference of the Active Site of DNA Gyrase. Synthesis of 10-Fluoro-6-methyl-6, 7-dihydro-9-piperazinyl-2 H-benzo …
…, S Pillai, A Keschavarz-Shokri, L Shen…
文献索引:Fecik, Robert A.; Devasthale, Pratik; Pillai, Segaran; Keschavarz-Shokri, Ali; Shen, Linus; Mitscher, Lester A. Journal of Medicinal Chemistry, 2005 , vol. 48, # 4 p. 1229 - 1236
In pursuit of an apparent literature anomaly, S-and R-6-methyl-6, 7-dihydro-2 H-benzo [a] quinolizin-2-one-3-carboxylic acids (12 and 22) were synthesized by an unambiguous route from optically active norephedrines, and their antibacterial potencies were measured. Against Gram-negative microorganisms and DNA gyrase a preference for S-absolute configuration was found whereas R-absolute stereochemistry was more active against ...