While continuing our investigation in improving the pharmaceutical activities of the local anesthetic Chinoxicaine we have studied the irreversible replacement of its 4-OH group for bioisosteric fragments. For this purpose the synthesis of a series of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids 2-(diethylamino)ethylamide hydrochlorides has been carried out. The experimental data of the local anesthetic properties of the compounds obtained are given and discussed.
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* For Communication 177, see [1].
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1050-1057, July, 2010.
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Ukrainets, I.V., Tkach, A.A., Kravtsova, V.V. et al. 4-hydroxy-2-quinolones. 178*. irreversible chemical modification of chinoxicaine at the position 4 of the quinolone ring. Chem Heterocycl Comp 46, 850–855 (2010). https://doi.org/10.1007/s10593-010-0593-z
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DOI: https://doi.org/10.1007/s10593-010-0593-z