901926-72-5Relevant academic research and scientific papers
5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation
Demina,Khodonov,Sinauridze,Shvets,Varfolomeev
, p. 2092 - 2113 (2015/06/08)
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 substituents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential antiaggregatory 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.
Novel Heterocyclic Compounds as Pesticides
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Page/Page column 23-24, (2012/04/23)
The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.
Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases
Bryant, Clifford,Kerr, Iain D.,Debnath, Moumita,Ang, Kenny K.H.,Ratnam, Joseline,Ferreira, Rafaela S.,Jaishankar, Priyadarshini,Zhao, DongMei,Arkin, Michelle R.,McKerrow, James H.,Brinen, Linda S.,Renslo, Adam R.
scheme or table, p. 6218 - 6221 (2010/06/19)
We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 A) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such analogs bind the S2 and S3 subsites of the protease, effectively recapitulating important binding interactions present in more traditional peptide-based protease inhibitors and natural substrates.
