Inhibition of DNA gyrase

Simon, H., L. Kittler, E. Baird, P. Dervan, and C. Zimmer Selective inhibition of DNA gyrase in vitro by a GC specific eight-ring hairpin polyamide at nanomolar concentration. FEBS Lett. 2000, 471, 173-176. 

Figure 6.2. Proposed model for quinolone-DNA cooperative binding in the inhibition of DNA gyrase [32], (Reprinted with permission American Chemical Society.)...

In another study concerning the conformational requirements of I-cyclopropyl-quinolones and their relationship to DNA gyrase inhibition, the conformation-ally constrained cyclopropane derivative (62), related to ofloxacin was prepared and evaluated in whole cells and for inhibition of DNA gyrase [95] the gem-dimethyl analogue (35), discussed earlier in the context of QSAR studies... 

Enhances inhibition of DNA gyrase (i.e., fluoroquinolones) No side effects... 

The antibacterial action of gatifloxacin result from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division. 

Inhibition of DNA gyrase, an enzyme required for DNA replication, transcription, repair and recombination in bacteria... 

The quinolones are rapidly bactericidal, largely as a consequence of inhibition of DNA gyrase and topoisomerase IV, key bacterial enzymes that dictate the conformation of DNA. The Escherichia coli chromosome is a single, circular molecule of approximately 1 mm in length, whereas the cell is only 1 to 3 pm long. Thus, the DNA molecule must be dramatically compacted in a conformationally stable way so that it... 

Quinolones are known antibacterial agents which represent a class of highly potent, broad-spectrum antibiotics. Their mode of action is believed to involve inhibition of DNA gyrase, and more recently they have been shown to have in vitro activity against M. Tuberculosis. ... 

Aminocoumarin antibiotics such as novobiocin, clorobiocin, and coumermycin A1 are derived from different Streptomyces species and show a very potent antibacterial activity by inhibition of DNA gyrase. Gyrase inhibitors block DNA replication, induce the SOS repair system, and eventually cause bacterial cell death (Figure 6.32) [151-154], These antibiotics possess a 3-amino-4-hydroxy-coumarin and a substituted deoxysugar noviose as common feature, which is essential for their biological activity. The biosynthetic gene clusters for novobiocin, chlorobiocin, and coumermycin A1 have been cloned in Streptomyces coelicolor M512 [155,156]. 

---