Related Experiment Video
Updated: May 31, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Synthesis and Na+/H+ exchanger inhibitory activity of benzoylguanidine derivatives
Lu Jin1, Xiang-Min Jiang, Ping Du
1Department of Medicinal Chemistry, China Pharmaceutical University, Tongjiaxiang 24, Nanjing 210009, China.
Abstract:
Twenty-two compounds of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Twelve compounds showed more potent NHE1 inhibitory activity than cariporide. The activities of compounds 7e, 7h and 7j (IC(50) = 0.073 ± 0.021, 0.084 ± 0.012 and 0.068 ± 0.021 nmol/L, respectively) were two orders of magnitude higher than that of cariporide (30.7 ± 2.5 nmol/L). Myocardial cells in vitro screening showed 7j had highlighted protective effect on cardiomyocytes subjected to hypoxia/reoxygenation. Thus it is valuable for further investigation.
Related Concept Videos
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...
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...
meta-Directing Deactivators: –NO2, –CN, –CHO, –⁠CO2R, –COR, –CO2H
Diazonium Group Substitution: –OH and –H
Drugs Affecting Neurotransmitter Release or Uptake
Inhibitors of Bacterial DNA Synthesis

