Sulphonamides and Sulfones: Handwritten Notes
Topics Covered:
- Historical development of sulphonamides and sulfones
- Chemistry and classification of sulphonamides
- Structure-Activity Relationship (SAR) of key sulphonamides:
- Sulphamethizole
- Sulfisoxazole
- Sulphamethizine
- Sulfacetamide*
- Sulphapyridine
- Sulfamethoxazole*
- Sulphadiazine
- Mefenide acetate
- Sulfasalazine
Detailed Explanation
Sulphonamides and sulfones are among the oldest classes of antimicrobial agents, playing a significant role in the history of medicine. This topic explores their historical development, chemical classification, and structure-activity relationship (SAR), providing insights into their therapeutic potential and limitations.
Historical Development: Sulphonamides were the first effective chemotherapeutic agents for bacterial infections. Introduced in the 1930s, they revolutionized the treatment of infectious diseases, significantly reducing morbidity and mortality.
Chemistry and Classification: Sulphonamides are characterized by the presence of a sulfonamide (-SO2NH2) functional group. Based on their pharmacokinetics and clinical applications, they can be classified into:
- Short-acting: Sulfisoxazole, Sulphamethizole
- Intermediate-acting: Sulphamethizine, Sulphadiazine
- Topical agents: Sulfacetamide, Mefenide acetate
- Combination agents: Sulfasalazine
Structure-Activity Relationship (SAR): The antimicrobial activity of sulphonamides depends on their ability to inhibit dihydropteroate synthase, a key enzyme in bacterial folate synthesis. Important SAR features include:
- A para-substituted aromatic ring for optimal activity
- A free sulfonamide group (-SO2NH2) essential for enzyme binding
- Electron-withdrawing groups to enhance potency and reduce toxicity
Sulfones: Compounds like Dapsone belong to the sulfone class and are used to treat leprosy and other chronic infections. They share a similar mechanism of action with sulphonamides but exhibit additional pharmacological properties.
In conclusion, sulphonamides and sulfones remain an integral part of antimicrobial therapy, with historical significance and continued relevance in treating specific infections.
Info!
If you are the copyright owner of this document and want to report it, please visit the copyright infringement notice page to submit a report.
