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Medicinal chemistry 2 5 th sem B PHARMACY
Q.1) Define anti-diabetic with classification, SAR & MOA
Q. 2) Define local anaesthetics with classification, SAR & MOA
Q. 3) Explain oral contraceptives
Q.4) Nomenclature of stereochemistry & metabolism of
steroids.
Q.5) Define anti-arrhythmic drugs with classification , MOA
SAR
Q.6) Define Antihyperlipidermic with classification
Q.7)Explain Coagulants & anticoagulants
Q. 8) Write a note on sex hormone.
Q.9) HMG-CoA reductase
Q. 10) Write a note on statins
Q. 11) Lovastatin
Q. 12) CHF (Congestive Heart Failure) SAR & MOA with
Classification
Q. 13) Antihypertensive drugs effects, classification
Q. 14) Classify diuretics with MOA
Q. 15) Write a note on "Gastrin Proton Pump Inhibitors
Q. 16) Write a note on calcium channel blocker, Vasodilator.
Q. 17) Define anti-neoplastic agents with classification & MOA
Q. 18) Define antihistamines with classification, moa, types,
SAR of antihistamines. H1 & H2 antagonist

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Q.1) Define anti-diabetic with classification, SAR & MOA
Anti-diabetic drugs-
The medicines which are used to stabilize and control
blood glucose level amongst peoples in diabetes called anti-
diabetic drugs.
Anti-diabetic drugs commonly used to manage diabetes
- There are different types of anti-diabetic drugs.
• Insulin
• Amylin
• Oral hypoglycaemic
MOA
1) For type 1 diabetes
• daily insulin essential
• type 1 diabetic patient must have to eat proper diet
• monitor glucose level regularly
• antidiabetic supress appetite
• -stimulate pancreas to secrete more insulin
2) For type 2 diabetes –
• diet & exercise enough to control diabetes
• Medicines taken orally oral hypoglycaemia) or injection
form (Insulin)
• Increase insulin secretion by pancreas
• Suppress appetite
 • SAR of anti-diabetic drugs

- must be bulk group on urea nitrogen

-only one substitution on sulfonyl aromatic ring
-Substitution may high potency"
Special relation bern amide nitrogen group &
sulphonamide nitrogen is important

Q. 2) Define local anaesthetics with classification, SAR & MOA

Local anaesthetics:-
The drugs which produce reversible loss of
sensation in local part of body called local anaesthetics .
* Classification:
Local anaesthetics
1 .Short duration 2. Intermediate duration 3. Longer duration
-Procaine - Lidocaine -Tetracaine
-Chloroprocaine - Prilocaine -Dibucain
*MOA of local anaesthetics
Local anaesthetics diffused through cell membrane
↓
Binds voltage gated Na channels
↓
Blocks Na + entry into cell
↓
No generation & conduction of impulse
↓
Produce local anaesthetic effect

• SAR
Q. 3) Explain oral contraceptives
- Oral contraceptives
These are (birth control pills) hormone containing
(progesteron, estrogen) medicines taken by mouth to prevent
pregnancy.

• MOA of oral contraceptives »

-prevent ovulation by inhibit folicular development
-contraceptives are combination of progesteron & estrogen
which prevent ovulation by providing negative feedback to
hypothalamic pituitary gland which stops sperm to entering
the uterus
• Side effects:-
- Headaches
- Nausea
↑B.P
- disturbance in periods bleeding

• Types of oral contraceptive pills

Combination pills
Progestin only pills
Continuous use pills
Q.4) Nomenclature of stereochemistry & metabolism of
steroids.
Nomenclature – Stereochemistry

• Metabolism of steroid
1.Primary metabolism of steroids takes place in liver where
first step involves reduction of double bond & introduction
of hydroxyl in A ring to form tetra hydro derivatives
2.orticosteroids metabolize through enzymatic
transformation.

• Types of steroids..

Tablet Prednisolone
Inhalers Baclometasone
Injection methylprednisolone
Creams Hydrocortisone
 • Corticosteroid produce in adrenal cortex
• Corticosteroid involves in - stress response,
- immune response
- carbohydrate metabolism
• Classification of corticosteroid
1. Natural -Glucocorticoid, mineral corticoid
2. Synthetic- Hydrocortisone, prednisolone, clobetasol

Q.5) Define anti-arrhythmic drugs with classification , MOA

SAR
Anti-arrhythmic drugs
The drugs which are used to prevent or treat
irregularities of cardiac rhythm
• Classification of anti-arrhythmic drugs
Class I :- Sodium channel blockers
Class II: B- Adrenergic blocker ex propranolol
Class III : Potassium channel blocker ex satolal
Class IV: Calcium channel blocker ex. Verapamil
Miscellaneous:- Digoxin, Atropine
MOA of anti- arrhythmic drugs
• Anti-arrhythmic drugs↓
Binds to sodium, sodium, potassium & calcium channels
↓ Blocks the action of sodium. potassium) & calcium
channels.
 ↓slow down heart electric impulse so heart beat comes to
normal.
* SAR of anti arrythmic drugs.

Q.6) Define Antihyperlipidermic with classification

Antihyperlipidermis agents.
- The agents which promote reduction of lipid level in the
blood.
Antihyperlipiderm low the - low density lipoprotein (LDL) - high
density lipoprotein (HDL) triglyceride levels
• Classification
1.HMG COA Reductase inhibitors – Lovastatin, simvastin
2) Fibrates Clofibrate, Ciprofibrate
3) LDL oxidation inhibitor – probucol
4) Pyridine derivatives – Nicotinic acid. Nicotinamide
5) cholesterol absorption inhibitors – Ezerimibe
6)Bile acid sequestrants – Cholestraymine, colestipol
7) Miscellaneous agents - B sitosterol. Dextrothyroxine
Q.7)Explain Coagulants & anticoagulants
Coagulants -These are drugs that promot coagulation and
control bleeding.
- They are also called as hemostatic agents
-They having two types - Systemis coagulants , Local coagulants
• Coagulation mechanisms
Prothrombin ----- Thrombin
Fibrin ------- Fibrinogen
Anticoagulants:-
These are agents that prevent clotting of blood when mixed
with blood in proper concentration
* Purpose of anticoagulants - -
-preservation of blood in blood bank
-Study various constituents of blood
* Properties of anticoagulants.
-Soluble in blood
- keep blood in fluid condition.
- Not change RBC size
-minimize aggrégation of platlets
*Warfarin & blood clotting (anticoagulants)
by blocking enzyme vitk
Q. 8) Write a note on sex hormone.
Female sex hormone – Progesterone
-Estrogen
-Male sex hormone.- Testosterone
* Functions of Progesteron & estrogen
1.Progesteron - regulation of menstrum cycle
. -preparation of body for pregnancy
2) Estrogen-breast development during pubirity
. uterine lining growth & bone strength maintenance
Functions of Testosterone
- increase bone density & muscle mass
-body hair growth
- voice deeping
-sexual & reproductive development

Q.9) HMG-CoA reductase

A substance that blocks an enzyme needed by the body to make
cholesterol & lower the amount of cholesterol in the blood.

HMG-CoA reductase acts in liver & control production of liver.

Q. 10) Write a note on statins
Statins:-These are effective at lowering cholesterol & promoting
against heart attack & Stroke.
They are mainly used to low cholesterol reduce risk of heart
attack or stroke
Cholesterol in blood comes from food, most made by liver
statins work by reducing amount of cholesterol made by liver
and helping liver remove cholestrol that Is already in blood.
Ex. Atrvastin. Lovastatin Pravastatin, Rosuvast

Q. 11) Lovastatin
Lovastatin is used together with a proper diet to lower
cholesterol & triglyceride (fat) levels in the blood.
This medicine may also help to prevent medical problems such
as chest pain, heart attack caused by fat clogging the blood
vessels.
Lovastatin should not take under 18 years children because liver
& kidney not develop in them.
Q. 12) CHF (Congestive Heart Failure) SAR & MOA with
classification
CHF (Congestive Heart Failure): It is condition in which heart
does not pump blood properlly
• Classification of CHF:
2) Stage A: High risk of hear failure, no symptoms.
3) Stage B: Structural heart disease, no symptoms
4) Stage C: Structural heart disease with symptoms

• MOA of CHF:
1.ACE inhibitors ↑ Vasodilation. ↓ workload of heart
2.Diuretics: removal excess water, salts & produce
metabolic products such as urea.
3.Glycosides it include digoxin ↑ force of contraction of
heart
4) B blockers. I activity (excessive) of sympathetic nerous
system which is characteristic of CHF

• SAR OF CHF
Q. 13) Antihypertensive drugs effects, classification
The drugs which are used to treat hypertension called
antihypertensive drugs.
• effects of antihypertensive drugs
Decrease BP,
- extra fluid & salt
- heartbeat (excessive to normal)
Q. 14) Classify diuretics with MOA
Diuretics:-
These are the agents which increases flow of urine at certain
level without causing dehydration
• Classification
 • MOA of diuretics

Renin release from kidney➔ Renin substrate ➔Angiotensin 1

Ace ↓
Angiotensin II
Binds ↓
Causes ← Angiotensin I receptor 2 receptor
↓
-Smooth muscle contraction
↓BP
↓preload on kidney
Q. 15) Write a note on "Gastrin Proton Pump Inhibitors
Gastrin Proton Pump Inhibitors:
They are used to control gastric acid & ulcer They acts on parital
cells of stomach.
Mechanism of Gastrin Proton Pump Inhibitors
Gastrin Proton Pump Inhibitor
↓
Binds to parital cells of stomach which responsible for Hcl
secretion
↓
Gastrin Proton Pump inhibitor having Sulphonyl group binds
with k’, H., ATP enzyme then they form drug enzyme complex
which further metabolite easily & inactive gastrin proton pump
↓
H+ ion production ↓
↓
HCl production ↓
↓
Blocks gastric acid secretion
Examples
Omeprazole, pantoprazole
Q. 16) Write a note on calcium channel blocker, Vasodilator.
Calcium channel blocker
These are medications used to lower B.P. They work by
preventing calcium from entering cells of heart & arteries.
Calcium causes the heart and arteries to contract more strongly
by blocking calcium, calcium channel blockers allow blood
vessels to relax & open.
Major effects of calcium channel blockers are relaxation of
vascular & arterial smooth muscle cells resulting in arterial
vasodilation.
ex- Amlodipine, Nifedipine

Vasodilator:

Vasodilators are agents which dilate blood vessels. They affect

on muscles in walls of arteries & veins, preventing muscles from
tightening & narrowing
Some vasodilators directly act on smooth muscle cells lining
blood vessels.
ex. Verapamil. Nifidipine
Q. 17) Define anti-neoplastic agents with classification & MOA
Anti-neoplastic agents -These are medications used to treat
cancer These drugs come in form of pills & liquids.
Anti-neoplastic agents targeting & killing rapidly dividing
cancerous cells They are also harmful for healthy dividing cells

MOA
CLASSIFICATION
Q. 18) Define antihistamines with classification, moa, types,
SAR of antihistamines. H1 & H2 antagonist
Antihistamines:
These are the agents which block the action of histamine by
binding to their receptors.
• Classification of antihistamines
H1 antagonist
Diphenhydramine HCl
-Chlorcyclizine HCl
Mecyclizine HCl n
- Buclizine HCl
Tripelemine HCL
2) H2 antagonist •
Gastric acid inhibitor
- Cimetidine -
- Ranitidine
- Famotidine
3) Gastric Protein Pump Inhibitor
- Omeprazole
Lansoprazole
Pantoprazole, - Rabeprazol
MOA of antihistamines:
-H1 antagonist acts on H1 receptor & inhibit effect of H1
receptor
-H2 antagonist acts on H2 receptor & inhibit effect of H2
receptor
- reduce allergic disorders
-reduce asthma
-sedative action
• Histamine receptor:-
There are four main histamine receptors H1, H2, H3, H4
H1. receptor
Location: Smooth muscle. Git track
Effect: Odemo, hypotension allergic reaction
-H2 receptor
location: Gastric parital cells. CNS. Heart, smooth muscle
-Effect- gastric acid secretion. Vasodilation
H3 receptor
location – CNS
-Effect: inhibit histamine release
H4 receptor -location: Hematopoietic cells
Effect- modulate immune system
SAR of antihistamine

Aryl group:
Phenyl & heterocyclic group ↑ activity
Methyl aryl group ↓ activity
Nature of x
☑ Nitrogen (N) Oxygen (0) Carbon (c) ↑ activity
x= Other than N. O. C ↓activity
Substitution on ethylene chain:
Ethylene chain ↑ activity
Branching of ethylene chain ↓activity
Promethazine is exceptional case
Amine group:
3 ° amine group ↑ activity
hetero cyclic ring 1 activity
• H1 antagonist:
Those agents which blocks Hi receptor & inhibit action of
histamine
These are of two types
1) 1st generation
2) 2nd generation

ex.
Diphenhydramine HCL
Triprolidine Hel
Promethazine HCl
Dimenhydramine
• H2 antagonist
Blocks H2 receptor present in stomach
- production of acid in stomach
Used in treatment of gastric acid & ulcer
-ex.
Cimetidine
Ranitidine
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