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9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
9 aminoacridine
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9 aminoacridine

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  • very nice ppt it helps me lot in my assignment .thanku Sir Khalid Hussain
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  • 1. 9-aminoacridinesAntimalarial drugs
  • 2. Acridines• Aacridine is formed when an additional benzene ring is fused with pyridine ring of quinoline nucleus. Acridine is overall aromatic, though having nitrogen Pyridine Quinoline Benzene
  • 3. 9-Amino acridine• has an amino group at C -9• It is a green fluorescent dye• In the past, the compound was used as an antiseptic for treating wounds infections
  • 4. Structure Activity Relationship• Various types of acridines were synthesized• Acridine has weak antiseptic and antibacterial activity• When a side chain – 2 amino, 5 diethylamino pentane- is introduced at C-9, the compound becomes antimalarial• When methoxy at position 2 and Cl at 6 are introduced –quinacrine- which is antimalarial• Quinacrine was the 1st synthetic agent that was used before quinolines
  • 5. 9 26 Quinacrine
  • 6. • When methoxy is shifted to position 6 and Cl to 2 (interchanged)-loss of antimalarial activity• When methoxy is replaced by ethoxy, toxicity is increased• When methoxy is rotated to any other position 1, 3, 4, then 50% activity is lost• When Cl is replaced with other halogens there is successive loss of activity
  • 7. • Side chain – 2 amino, 5 diethylamino pentane- has no antimalarial activity but when attached to aromatic system the compound became antimalarial• When at position-1, a N is introduced – azacrine- which has good antimalarial activity and rapid onset of action
  • 8. Azacrine
  • 9. • A very useful drug was taken from quinacrine by Gemans by separating it into two halves;• 1 half chloroquine active• 2 half was inactive
  • 10. Chemical synthesis (p-methoxy aniline)2, 4 dichloro benzoic acid Condensation reaction
  • 11. -HCl2, p-methoxy phenyl amino, 4 chloro benzoic acid
  • 12. POCl36- chloro , 2-methoxy acredinone
  • 13. POCl36, 9 dichloro, 2-methoxy acredine
  • 14. 26 chloro, 9 diethylaminopentyl, 2-methoxy, acredine
  • 15. Therapeutic uses• Treating erythrocytic stage of malaria• Earlier, was used in treating black water fever• Have anthalmentic activity against intestinal parasites• It is eliminated slowly and have side effects
  • 16. Non-therapeutic use• Being green fluorescent dye, used to visualize blood cells, particularly platelets• Platelets store the dye in dense granules
  • 17. Side effects• Gastric irritation• Staining of tongue and skin

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