5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives.

doi:10.1021/jm00121a010

Paper

5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives.

Published 1989 · A. Morikawa, T. Sone, T. Asano

Journal of medicinal chemistry

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Abstract

Two novel series of N-(2-guanidinoalkyl)-5-isoquinolinesulfonamides, 2 and 3, were prepared. Many of the compounds possessed vasodilatory activity when injected locally into the femoral artery of dogs. The most potent compound, 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiazepine, 33, was comparable to diltiazem, which is used clinically as a vasodilator.

Study Snapshot

N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives show vasodilatory activity, with the most potent compound being 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiaze

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives.

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References

Citations

Paradoxically, Most Flexible Ligand Binds Most Entropy-Favored: Intriguing Impact of Ligand Flexibility and Solvation on Drug-Kinase Binding.

The most flexible ligand exhibits the most favored binding due to its ability to efficiently entrap water molecules in solution before protein binding, rather than increased residual flexibility or water release.

KN-62 analogues as potent differentiating agents of HL-60 cells.

KN-62 analogues, such as AS-004, show potential in inducing differentiation of HL-60 cells, potentially benefiting treatment of promyelocytic leukemia.

Synthesis, Biological Activity and Molecular Modeling Studies of 1,2,3,4-Tetrahydroiso-quinoline Derivatives as Conformationally Constrained Analogues of KN62, a Potent Antagonist of the P2X7-Receptor Containing a Tyrosine Moiety

The new series of 1,2,3,4-tetrahydroisoquinoline derivatives show weak antagonistic activity at the P2X7 receptor, with extended conformation being crucial for antagonistic activity.

Modulation of cellular processes by H7, a non-selective inhibitor of protein kinases

H7 is a less effective inhibitor of protein kinases than staurosporine, making it unsuitable for studying PKC involvement in cellular processes.