Antihypertensive thiadiazoles. 1. Synthesis of some 2-aryl-5-hydrazino-1,3,4-thiadiazoles with vasodilator activity.

doi:10.1021/JM00400A003

Paper

Antihypertensive thiadiazoles. 1. Synthesis of some 2-aryl-5-hydrazino-1,3,4-thiadiazoles with vasodilator activity.

Published May 1, 1988 · S. Turner, M. Myers, B. Gadie

Journal of medicinal chemistry

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104

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0

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Abstract

Some 2-aryl-5-hydrazino-1,3,4-thiadiazoles have been synthesized and screened for antihypertensive activity. In general, compounds with a 2-substituted phenyl ring had higher activity than their 3- or 4-substituted counterparts or those containing heteroaryl groups. The 2-methylphenyl and 2-ethylphenyl derivatives 7 and 18 were the most potent members of the series. Preliminary studies indicated that the hypotensive action of these compounds was due to a direct relaxant effect on vascular smooth muscle.

In Vitro Study

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Study Snapshot

2-aryl-5-hydrazino-1,3,4-thiadiazoles with 2-substituted phenyl rings show antihypertensive activity, likely due to a direct relaxant effect on vascular smooth muscle.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Antihypertensive thiadiazoles. 1. Synthesis of some 2-aryl-5-hydrazino-1,3,4-thiadiazoles with vasodilator activity.

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References

Citations

Rational design, synthesis, and anti-cancer evaluation of amide derivatives of 1,3,4-Thiadiazole benzimidazoles

The amide derivative 13a of 1,3,4-thiadiazole-benzimidazole shows potent anticancer activity against human breast, lung, colon, and ovarian cancers.

Multitarget Pharmacology of Sulfur–Nitrogen Heterocycles: Anticancer and Antioxidant Perspectives

Sulfur-nitrogen heterocycles show potential as dual antioxidant and anticancer drugs, potentially enhancing therapeutic efficacy in oncology by targeting multiple pathways.

Antimicrobial and Molecular Docking Studies of 1,3,4-Thiadiazole Tethered Sulfa-Azo Derivatives via Hydrazono-Methyl Bridge

The 1,3,4-thiadiazole compounds 3k and 3l show potent antimicrobial activity against various bacteria, with 3k showing a notable effect on destroying microbial cell walls and binding to dihydropteroate synthase enzymes.

1,3,4- Thiadiazole and Its Derivatives- A Review on Syntheic Account and Recent Progress on its Phermoacological Activities

1,3,4-thiadiazole and its derivatives exhibit diverse biological activities, making them significant scaffolds in various pharmaceutical categories.

Rational design, synthesis, and anticancer evaluation of amide derivatives of Pyridin3-yl)imidazo[2,1-b][1,3,4]thiadiazole linked 1,3,4-oxadiazoles

Most of the new amide derivatives of pyridin-3-yl)imidazo[2,1-b][1,3,4]thiadiazoles show excellent to moderate anticancer activity against various human cancer cell lines.

Design, synthesis and anticancer evaluation of aryl pyrimidine-thiadiazoles

Compounds 8a, 8d, 8e, 8f, and 8g show potent anticancer activity against various human cancer cell lines, with compound 8e showing particularly remarkable activity.

Design, synthesis, anticancer evaluation, molecular docking and in silico ADME analysis of novel substituted 1,3,4-thiadazoloaryl incorporated pyrimidine-thiazole derivatives as propitious anticancer agents

Novel 1,3,4-thiadazoloaryl based pyrimidine-thiazole derivatives show promising anticancer activity, with some showing more prominent activity than etoposide.