| Autor: |
K E, Frank, P V, Devasthale, E J, Gentry, V T, Ravikumar, A, Keschavarz-Shokri, L A, Mitscher, A, Nilius, L L, Shen, R, Shawar, W R, Baker |
| Rok vydání: |
1999 |
| Předmět: |
|
| Zdroj: |
Combinatorial chemistryhigh throughput screening. 1(2) |
| ISSN: |
1386-2073 |
| Popis: |
A series of pure fluoroquinolone antiinfective agents was prepared by multiple parallel synthesis using a simple new apparatus. These compounds were evaluated biologically against Gram-positive and Gram-negative microorganisms and against a BCG strain transfected with luciferase in a fluorescence-based antitubercular assay. Activity against relatively fast growing, acid-fast Mycobacterium smegmatis was determined in part by agar-dilution streak assays. Data obtained against Escherichia coli-derived DNA gyrase does not correlate well with whole cell assays against E. coli. These compounds were assayed by a convenient glass-fiber filter binding method modified for high throughput screening. In these analogs, the results with a N-1 cyclopropyl substituent were often inferior to those obtained with a N-1 2',4'-difluorophenyl substituent. None of the new compounds prepared was superior in its antimycobacterial potency to ciprofloxacin or temafloxacin. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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