Synthesis and pharmacological activities of 7-azaindole derivatives
Nousheen Mushtaq1, Z S Saify, Fozia Noor
1Department of Pharmaceutical Chemistry, University of Karachi, Karachi-75270, Pakistan. noshin_mushtaq@yahoo.com
Abstract:
As a part of our program to discover novel analogues of 7-azaindole (1H-Pyrrolo[2,3-b] pyridine) having useful biological activities, some derivatives have been synthesized and evaluated for their analgesic and hypotensive activity. Compounds evaluated by thermal stimuli (tail immersion method) at the dose of 50 mg/kg of body weight revealed significant analgesic activity. Pethidine was used as reference drug. Same compounds tested at the dose of 75 mg/kg of body weight showed toxicity. Compounds tested for their effect on blood pressure in normotensive rat produced slight fall in blood pressure.
More Related Videos
Related Concept Videos
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Adrenergic Agonists: Indirect-Acting Agents
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...


