Fimasartan ARBs

2. Kanarb
Brand-name.
2-(1-((2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-
methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-N,N- dimethylethanethioamide
Chemical-name.

3. |Chemicalstructure byMARVIN.

4. |Chemical structuredrawnbyMARVINsketch.

5. |Chemicalsynthesis.

6. |Chemical synthesis.
4-[2'-(N-triphenylmethyltetrazol-5-
ylphenyl]benzylbromide
Thioamidation
Acidic media
+ Basic Media
1 2
Fimasartan
2-(1-((2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-
yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-
dihydropyrimidin-5-yl)-N,N-
dimethylethanethioamide
3
4

7. |MedicalUsesofthedrug.

8. Heart
|Medical Usesofthedrug.
Failure

9. |Mechanism ofaction.

10. NORMAL.Blood pressure and fluid and electrolyte homeostasis is regulated by the
Renin–Angiotensin–Aldosterone System
Renin - enzymereleased fromthekidneys-
Angiotensinogen
angiotensin I Angiotensin IIAngiotensinConvertingEnzyme
AT1 receptor
cardiaccontractility
sodiumreabsorption
vasoconstriction
Increase Blood Pressure
Increase noradrenaline release

11. DRUG.ARBs are blocking the last part of the renin–angiotensin pathway by
blockingAT1 receptorsand lead to lower bloodpressure
Decrease
Renin - enzymereleased fromthekidneys-
Angiotensinogen
angiotensin I Angiotensin IIAngiotensinConvertingEnzyme
AT1 receptor
cardiaccontractility
sodiumreabsorption
vasoconstriction
Increase Blood Pressure
Decrease noradrenaline release
XX

12. |Pharmacokinetics.

13. |Pharmacokinetics.
• Rapidly absorbed and has minimal accumulation in the body 7 days after administration
• Half-life of 7 to 10 hours
• Effective in fasted or fed states, with a variety of dosing regimens.
• Reach the maximum plasma concentration after 30 minutes to 3 hours after dosing.
• Most is eliminated un-changed in bile with less than 3% in the urine

14. |StructureActivityRelationship.

15. Acidic group like Tetrazole
must be in the ortho position for optimal activity
Lipophilicity, and oral bioavailability
Metabolism
|StructureActivityrelationship.

16. N-butyl group of model compound
Provides Lipophilic binding
Mimics the side chin of Angiotensin II
|StructureActivityrelationship.

17. High Lipophilicty
|StructureActivityrelationship.
Absorption

18. Activity
|StructureActivityrelationship.
Activity
Contains Valine Mimics the side chin of Angiotensin II
Fimasartan Valsartan

19. THANK YOU