SAR of Antihistamines || Most Important For Drugs structure || L-2, Unit-1 || Medicinal chemistry-2

In this Video we Cover,

UNIT- 1

:- SAR of Antihistamines / H1 Antagonist / Antiallergic


Subject- Medicinal chemistry-2
BPharm- 5th semester


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DEFINATION,

1. What is H1 Antagonist?

The drugs that competitively binds to the H1 receptor and inhibits the action of histamine on H1 receptor are called H1 Antagonist / H1 receptor blockers.

2. Structural Activity Relationship (SAR):

SAR of any drug is studied based on the modification done in the general structure of the drugs belonging to same category.

So the general structure of H1 Antagonist given in this lecture.

The structure is divided into four parts:

The Aryl group
Nature of ‘X’
The alkyl chain (The carbon chain)
The terminal Nitrogen.
1.)The Aryl group:

Ar = Aryl group including phenyl and heteroaryl group.

Ar’ = Aryl group or aryl methyl group.

Sometimes, the two aromatic ring are bridged, which Constituents tricyclic derivatives.

2. Nature of ‘X’

Here ‘X’ does not represent halogen but here the ‘X’ could be oxygen (O) , Carbon (C) , or Nitrogen (N).

‘X’ provides basis of classification of antihistamines.

When ‘X’ = O it is aminoalkyl ether

When ‘X’ = C it is mono aminopropyl analogue

When ‘X’ = N it is ethylene-diamine derivative.


3. Alkyl chain (carbon chain):

Most of the antihistamines contains ethylene chain.

4. The terminal Nitrogen

The terminal Nitrogen should be 3° amine for the maximum activity.

The terminal Nitrogen can be the part of heterocyclic ring and still it retains high antihistamine activity.

e.g: chlorcyclizine


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Queries:-

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