Related Experiment Video
Updated: Aug 15, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Structure-activity relationships of some indolo[3,2-c]quinolines with antimalarial activity
1Department of Pharmacy, National University of Singapore, 10, Kent Ridge Crescent, Singapore, Republic of Singapore 119260.
Abstract:
The synthesis, physicochemical characterization and in vitro antimalarial activity of a series of indolo[3,2-c]quinolines (9a-f) are described. There is only a poor correlation between the activity and hydrophobicity. In contrast, 33% of the observed variation in antimalarial activity can be attributed to the size of the side chain attached to position 9 of the indoloquinoline ring. An increase in the size of this dibasic side chain generally results in a reduction in activity, suggesting that it is accommodated in a site/cavity of limited size on the receptor. More significantly, the charge on the distal nitrogen (N3) on the side chain, located 10-11 A from the quinoline N, could account for 75% of the observed variation. Since a large charge on N3 is associated with improved antimalarial activity, it is suggested that N3 is protonated and functions as a H bond donor in the drug-receptor interaction.
More Related Videos
07:30A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones
Published on: January 21, 2020
10:24Identification of Potential Anti-TB Candidates: A Step-by-Step Guide to Synthesis, MIC Determination, and Cytotoxicity Assessment in Mammalian Cells
Published on: May 22, 2026
Related Concept Videos
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
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...
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Anthelminthic Agents
Antiprotozoal Agents
Inhibitors of Bacterial DNA Synthesis