Medicinal Chemistry-2 of B-Pharmacy

1. Reporter:Gourav singh
Medicinal Chemistry-2
Gourav Singh 1

2. content
1.Introduction
2.Classification
3.Mechanism of Action
4.Types
5.Study of Individual Drugs
Gourav Singh 2

3. 1.
Introduction
Gourav Singh 3

4. Coagulant
Blood coagulation is an important biochemical
reaction which ensures the cessation of blood
loss from the damaged blood vessels.
Coagulation is an important part of the
hemostatic mechanism. Disorders of blood
coagulation result to excessive hemorrhage
and/or thrombosis and embolism.
Coagulants help in blood coagulation and are
indicated in hemorrhagic conditions. The
elements or factors required for coagulation are
found in the fresh whole blood or plasma and
are therefore indicated in case of deficiency of
any clotting factor.
Anticoagulant
Blood coagulation is a complex process in which
blood forms solid clots. It is essential part of
hemostasis in which a damaged blood vessel
wall is enclosed by a fibrin clot to prevent
hemorrhage and to repair the damage d vessel.
Disorders of blood coagulation increase the
occurrence of hemorrhage and/or thrombosis and
embolism.
Gourav Singh 4

5. 2.
Classification
Gourav Singh 5

6. The coagulants are classified as follows:
1) Vitamin K
i) K1 (from plants, fat-soluble): Phytonadione
(Phylloquinone).
ii) K3 (synthetic)
a) Fat-Soluble: Menadione and
Acetomenaphthone.
b) Water-Soluble: Menadione sodium
bisulfite and Menadione sodium diphosphate.
2) Miscellaneous: Fibrinogen (human), Anti-
haemophilic factor, Desmopressin, Adrenochrome
monosemicarbazone, Rutin, and Ethamsylate.
Anticoagulants are classified as follows:
1) Coumarin Derivatives
1. Warfarin
2. Dicoumarol
3. Phenprocoumon
4. Acenocoumarol
2) 3-Indanedione Derivatives
1. Phenindione
2. Anisindione
3. Bromindione
4. Diphenadione
Gourav Singh 6

7. 3.
MOA
Gourav Singh 7

8. Gourav Singh 8

9. 4.
Types
Gourav Singh 9

10. This pathway starts with events taking place in the
lumen of blood vessels. The intrinsic pathway
utilise the elements present in or intrinsic to the
vascular system. Such elements include clotting
factors, Ca++, platelet surface, etc.
Intrinsic Pathway
Coagulation is initiated by any of the two pathways:
This pathway utilise tissue thromboplastin (tissue
factor), which is a substance extrinsic to or not
found circulating in the vessel. A ruptured vessel
wall releases the tissue factor.
Extrinsic Pathway
Gourav Singh 10

11. 5.
Study of Individual
Drugs
Gourav Singh 11

12. IUPAC Name: 2-methylnaphthalene-1,4-dione
Properties: It occur as bright yellow crystal, insoluble in water. It has very faint acrid
acid. It get metabolized in liver by glucuronidation to give inactive metabolites.
Mechanism of Action: It is a vitamin k3 and is involved as a cofactor in the
carboxylation of glutamic acid residues of certain protein in the body. These protein
are vitamin K dependent coagulation factors II, VII, IX and X.
Uses:
1. It is used in treatment of hypothrombinemia
2. It is used in nutritional supplement in animal feed as it has some vitamin K
activity.
1. Menadione
The following coagulants are discussed below:
1) Menadione, and
2) Acetomenadione.
Gourav Singh 12

13. IUPAC Name: (4-acetyloxy-3-methylnapthalen-1-yl)acetate
Properties: It is white solid, very soluble in water and is stable under normal
temperature and pressure. It must be stored in tightly closed in container.
Mechanism of Action: It maintain normal blood clotting and act by reducing
excessive bleeding
Uses:
It is used to treatment of coagulation disorder due to vitamin K deficiency.
2. Acetomenadione
Gourav Singh 13

14. IUPAC Name: (RS)-4-hydroxyl-3-(3-oxo-1-phenylbutyl)coumarin
Properties: It is white solid, very soluble in water. It is hygroscopic in nature. It is
metabolised in the liver and kidney.
Mechanism of Action: It decrease the synthesis of prothrombin factor, VII, IX and X
by antagonizing the effect of vitamin k.
Uses:
It is used in treatment of deep veinthrombosin
Used as an anticoagulant and reduce the risk of embolism.
1. Warfarin
The following anticoagulants are discussed below:
1) Warfarin,
2) Anisindione, and
3) Clopidogrel
Gourav Singh 14

15. 1. Warfarin
Synthesis:
Gourav Singh 15

16. IUPAC Name: 2-(-p-methoxy-phenyl)indan-1,3-dione
Mechanism of Action: It is used in treatment of deep veinthrombosinIt reduce
synthesis of active coagulation factor like II, VII, IX, and X along with anticoagulation
protein C and S
Uses:
Used as an anticoagulant
Used in prevention and treatment of venous thrombosis, pulmonary embolism,
coronary, occlusion.
1. Anisindione
Gourav Singh 16

17. IUPAC Name: (+)(s)-methyl-2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-
C]pyridin5(4H)-yl)acetate
Properties: It is white crystalline powder, sparingly soluble in water. It get
metabolised in liver by hydrolysis to give inactive metabolite.
Mechanism of Action: It inhibit platelet aggregation by blocking the G1-coupled
platelets ADP receptors. It is a prodrug and it activated by the help of cytochrome
enzyme. On activation it irreversible binds and inhibit ADP receptors which involved
in the activation of platelets and their aggretion
Uses:
Used as an antiplatelets drug to reduce the risk of heart failure and stroke.
1. Clopidogrel
Gourav Singh 17

18. THANK
YOU
Gourav Singh 18