The document discusses the structure-activity relationship of quinolones, highlighting how various positions on the quinolone molecule influence its potency, pharmacokinetic profiles, and activity against bacteria. Key positions are identified as critical for functions such as gyrase binding, controlling antibacterial potency, and affecting specific activity against certain bacterial types. Overall, the document emphasizes the importance of structural modifications in enhancing the effectiveness of quinolones.

1. Structure
Activity
Relationship
QUINOLONES.

2. 2
3
4

3. (I) First position resonsible for potency and pharmacokinetic profile .
(ii) At second position contain limited alterations .
(iii) 3rd and 4rt Position resonsible for essential for gyrase binding and
bacteial membrane transport .
(iv) 5th position resonsible for GRAM + potency influence and as well as
it influences phototoxicity ( skin irritation ) .
(v) 6th position resonsible OR active controlling gyrase (bacterial -
- enzyme) and antibacterial potency .

4. (vi) 7th position responsible for both spectrum of activity and
As well as pharmacokinetic profile controlled .
(vii) At 7th position ''5'' and ''6'' memberd ring containing
''N'' atom yield the excellent activity .
(viii) 7th position controlled GABA binding .
(IX) 8th position responsible for specifc activity against
anaerobic bacteria can be adjusted from this point .
(X) etc …....!