期刊
RUSSIAN CHEMICAL BULLETIN
卷 71, 期 9, 页码 1969-1975出版社
SPRINGER
DOI: 10.1007/s11172-022-3615-y
关键词
4H-pyrrolo[3; 2; 1-ij]quinoline-1; 2-dione; thiosemicarbazide; condensation; thiazole; anticoagulant activity; factor Xa; factor XIa
资金
- Russian Science Foundation [18-74-10097]
A series of novel compounds were obtained through a reaction, and these compounds exhibit good anticoagulant activity against blood clotting factors Xa and XIa.
A reaction of 2-(4,4,6-trimethyl-2-oxo-4H-pyrrolo[3,2,1-ij]quinoline-1-ylidene)-hydrazinocarbothioamides with alpha-halocarbonyl compounds, such as ethyl bromocetate and 2-bromoacetophenone derivatives, afforded a series of novel 4,4,6-trimethyl-2-oxo-4H-pyrrolo[3,2,1-ij]quinoline-1(2H)-ylidene)hydrazinylidene)thiazolidin-4-ones and 4,4,6-trimethyl-1-(2-(4-arylthiazol-2-yl)hydrazinylidene)-4H-pyrrolo[3,2,1-ij]quinolin-2(1H)-ones. The synthesized compounds exist in the form of Z-isomers. Primary screening in vitro of inhibitory activity towards blood clotting factors Xa and XIa was carried out, revealing that the thiazole derivative bearing the 4-chlorophenyl substituent at the thiazole moiety exhibits a sufficiently high anticoagulant activity towards these blood clotting factors.
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