Topic
Fostedil
About: Fostedil is a research topic. Over the lifetime, 25 publications have been published within this topic receiving 277 citations.
Papers
TL;DR: The present study indicates that the existence of an aromatic ring substituted thiazole ring and the presence of phosphonate at an appropriate distance from the thiazoles ring are important for the coronary vasodilator action of fostedil.
Abstract: Structural modification and the coronary vasodilator activity of the calcium antagonist fostedil (KB-944) are described. Elimination of the bezothiazole ring or replacement of the benzothiazole ring of fostedil with other hetero rings leads to a decrease in vasodilator activity. Change of the distance from the aromatic ring to the phosphorus of fostedil causes a decrease in the activity. The present study indicates that the presence of an aromatic ring substituted thiazole ring and the presence of phosphonate at an appropriate distance from the thiazole ring are important for the coronary vasodilator action of fostedil.
52 citations
TL;DR: In this article, two crystal forms of fostedil were characterized using X-ray diffraction patterns and infrared spectra, and the melting points of polymorph I and II were 95.3 °C and 96.4 °C, respectively.
Abstract: Two crystal forms of fostedil were characterized using X-ray diffraction patterns and infrared spectra. The melting points of polymorph I and II were 95.3 °C and 96.4 °C, respectively.Solubility studies demonstrated that, of the two fostedil polymorphs, form II was slightly more soluble than form I. The free energy difference between two polymorphs was small (71.8 cal/mol at 37 °C). Both crystals melted at about 60 °C in water considerably below the melting points.Compression of form II at a compression force of 500 - 1000 kg/cm2 induced polymorphic changes in the crystal. Similar changes also were produced through grinding. The effects of some diluents on the polymorphic transformation from form II into form I by grinding were also studied. Microcrystalline cellulose and corn starch showed a polymorphic transfomation-accelerating effects.Form I is more suitable for the pharmaceutical preparation.
35 citations
TL;DR: Several p-substituted diethyl benzylphosphonates related to the calcium antagonist Diethyl 4-(2-benzothiazolyl)benzylphophosphonate (fostedil) have been studied as discussed by the authors.
30 citations
TL;DR: In this article, a regio specific synthesis of 5-fluorobenzothiazoles was accomplished by using difluorothiobenzanilides as a key intermediate.
19 citations
TL;DR: Structural modifications of the calcium antagonist fostedil (KB-944) and their coronary vasodilator activity are described and the 2-oxopyrrolidine derivative 7a was the most effective compound.
Abstract: Structural modifications of the calcium antagonist fostedil (KB-944) and their coronary vasodilator activity are described. Amidophosphonates 4a-m, lactam amidophosphonates 7a-1, and diamide dilactam 10 were prepared, and their coronary vasodilator activity was assessed in dogs. Many compounds exhibited coronary vasodilator activity superior to that of fostedil. Among them, the 2-oxopyrrolidine derivative 7a was the most effective compound. Its action as a coronary vasodilator was 3 and 2 times more potent than that of fostedil and diltiazem hydrochloride, respectively.
18 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2004 | 1 |
| 1994 | 4 |
| 1993 | 1 |
| 1992 | 4 |
| 1991 | 1 |
| 1990 | 4 |