Comparison of anti-aggregatory activities of 5-phenyl-3-(3-pyridyl)isoxazole and 5-phenyl-3-(3-pyridyl)-1,2,4-oxadiazole

Demina, O. V.; Лаптев, А. В.; Lukin, Alexey; Khodonov, A. A.; Belikov, N. E.; Fomin, M. A.; Gribkova, Irina V.; Швец, В. И.; Варфоломеев, С. Д.

doi:10.1134/s1990747811030032

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“…The TP receptor antagonist GB32191B did not suppress the first wave of ADP and adrenaline in duced aggregation either. 45 High Hill coefficients may also be typical for the receptor antagonists involved in the signal transduction at the beginning or in the middle of signal pathway, apart from elucidation of the supercooperativity stage (as in the case of indomethacin).…”

Section: Study Of the Mechanism Of Action Of 35 Disubstituted Isoxazmentioning

confidence: 98%

“…45 While investigating the effect of the test compounds on the platelet aggregation, we deter mined the following kinetic parameters: the maximum rate of aggregation (V max ) and the maximum degree of aggregation (A max ) ( Fig. 1, a).…”

Section: Antiaggregatory Activity Of 5 Substituted 3 Pyridylisoxazolementioning

confidence: 99%

“…1 After the analysis of published data, we chose a combi nation of pyridine and isoxazole moieties as the basic struc ture for the synthesis of antiaggregatory agents. 45 We syn thesized a number of new 3,5 disubstituted isoxazoles and revealed the presence of antiaggregatory activity. [45][46][47][48][49] Re lying on analysis of published data, we assumed that these compounds could act as thromboxane synthase inhibitors or TP receptor antagonists.…”

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confidence: 99%

“…45 We syn thesized a number of new 3,5 disubstituted isoxazoles and revealed the presence of antiaggregatory activity. [45][46][47][48][49] Re lying on analysis of published data, we assumed that these compounds could act as thromboxane synthase inhibitors or TP receptor antagonists. Prostanoids possess a very broad spectrum of activity; 1,50-53 therefore, earlier, it was believed that substances with this type of activity are need ed only for fundamental research of signaling pathways.…”

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confidence: 99%

“…5,21,37-44 Although a number of known medicaments are used for the treatment of cardiovascular diseases, the development of new nonsteroidal antiaggregatory agents with less side effects based on heterocycles is of inter est. 2, 45 The development of both selective TP receptor antagonists and dual action antiaggregatory compounds affecting both the TP receptor and the thromboxane syn thase are most important. A minor number of thromb oxane synthase inhibitors and TP receptor antagonists are currently clinically used to prevent a number of cardio vascular disorders.…”

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5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation

et al. 2014

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A series of 5 substituted 3 pyridylisoxazoles were synthesized using [3+2] cycloaddition of nitrile oxides to alkynes with variation of substituents at position 5 of the isoxazole ring without additional synthetic stages and with retention of 2 pyridyl , 3 pyridyl, and 4 pyridyl substitu ents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential anti aggregatory agents showing in vitro activity in the concentration range from 1•10 -6 mol L -1 to 1•10 -4 mol L -1 toward the human platelet rich blood plasma with arachidonic acid being used as the inductor of aggregation. These compounds do not act as cyclooxygenase or thromboxane synthase inhibitors, nor as thrombin inhibitors.

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Section: Study Of the Mechanism Of Action Of 35 Disubstituted Isoxazmentioning

confidence: 98%

Section: Antiaggregatory Activity Of 5 Substituted 3 Pyridylisoxazolementioning

confidence: 99%

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