ChemInform Abstract: SYNTHESIS OF 3‐DIALKYLAMINOPROPYL‐2‐THIOHYDANTOIN DERIVATIVES AS POTENTIAL ANTIARRHYTHMIC AGENTS

Ryczek, J.; Kusowska, J

doi:10.1002/chin.198352193

Cited by 1 publication

(2 citation statements)

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“…Similarly to epanutin and quinidine, these compounds did not protect the heart from single ventricular premature beats, but reduced the bigeminy and salvos calculated according to Bernauer [21] . Table 2 gives the data describing pharmacological activity in chloroform-induced arrhythmia published for all but two compounds (7,8) earlier. The references are also included in Table. It can be noticed that compounds 1 and 5 show the highest activity in vivo, similarly as indicated by the arrhythmia severity index calculated for in vitro tests.…”

Section: Ventricular Arrhythmias Associated With Coronary Artery Occlmentioning

confidence: 99%

“…However its limited clinical effectiveness and side effects [1] induced several authors to synthesise numerous derivatives which proved to have antiarrhythmic activity [3][4][5][6][7][8][9] . Since hydrophilic character is essential for the activity of antiarrhythmic agents [1] it was necessary to design a synthesis of DPH derivatives which would change the original lipophilic properties of the parent compound.…”

Section: Introductionmentioning

confidence: 99%

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Structure-Activity Relationship of Some New Anti-Arrhythmic Phenytoin Derivatives

Ciechanowicz-Rutkowska

Stadnicka

Kieć‐Kononowicz

et al. 2000

Arch. Pharm. Pharm. Med. Chem.

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The pharmacological activity of nine anti‐arrhythmic phenytoin derivatives was assessed in preventing chloroform‐induced arrhythmia. The compounds were tested in vitro on isolated heart of the rat. Four compounds were chosen as representative of the spatial characteristics of the studied group, and X‐ray structure analyses were carried out on them. Because the protonated form is present in physiological milieu, conformational analysis was performed on the protonated form of the four representatives and in addition on the compound showing the highest anti‐arrhythmic activity. It was found that substitution of the imidazolidinone ring of phenytoin at position 3 by a chain containing a tertiary amine nitrogen atom changes the affinity profile from inactivated (phenytoin‐like) to activated (quinidine‐like) cardiac sodium channels. The activity of the studied compounds relies on the presence of protonated tertiary nitrogen atom, at least one phenyl ring, and flexibility of the molecule, which enables the spacer to assume a desired length.

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Section: Ventricular Arrhythmias Associated With Coronary Artery Occlmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Structure-Activity Relationship of Some New Anti-Arrhythmic Phenytoin Derivatives

Ciechanowicz-Rutkowska

Stadnicka

Kieć‐Kononowicz

et al. 2000

Arch. Pharm. Pharm. Med. Chem.

View full text Add to dashboard Cite

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ChemInform Abstract: SYNTHESIS OF 3‐DIALKYLAMINOPROPYL‐2‐THIOHYDANTOIN DERIVATIVES AS POTENTIAL ANTIARRHYTHMIC AGENTS

Abstract: Durch Kondensation von Isothioeyunuten (I) mit Aminosiiiiren (II) werden Thiohydantoine (III) erhalten.

Cited by 1 publication

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Structure-Activity Relationship of Some New Anti-Arrhythmic Phenytoin Derivatives

Structure-Activity Relationship of Some New Anti-Arrhythmic Phenytoin Derivatives

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