- Synthesis of novel 5-aryl-2-thio-1,3,4-oxadiazoles and the study of their structure-anti-mycobacterial activities
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The preparation of novel 5-aryl-2-thio-1,3,4-oxadiazoles 4a-41 and the computer-aided study of their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) are reported. The average accuracy of the electronic-topological method and neural network methods applied to the activity prediction in leave-one-out cross validation is 80%.
- Macaev, Fliur,Rusu, Ghenadie,Pogrebnoi, Serghei,Gudima, Alexandru,Stingaci, Eugenia,Vlad, Ludmila,Shvets, Nathaly,Kandemirli, Fatma,Dimoglo, Anatholy,Reynolds, Robert
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p. 4842 - 4850
(2007/10/03)
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- The reaction of 5-aryl-(hetaryl)-2-aroylmethylthio-1,3,4-oxadiazoles with aryldiazonium tetrafluoroborates
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5-Aryl(hetaryl)-2-aroylmethylthio-1,3,4-oxadiazoles behave as CH acids and readily react with aryldiazonium tetrafluoroborates at the active methylene group to give azo coupling products. The spectroscopic properties of the compounds synthesized have been
- Krasovsky,Andrushko,Demchenko
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p. 496 - 499
(2007/10/03)
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- Ring Transformation of 1,3,4-Oxadiazole to s-Triazole-Fused Heterocycles. New Synthetic Route for Thiazolo-s-triazole and 7H-s-Triazolothiadiazine
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s-Triazole-fused heterocycles have been synthesized by an intramolecular transformation of some 1,3,4-oxadiazole ketones with ammonia or hydrazine.The α- ketone 2m gave thiazolo-s-triazole (4m), accompanied by a small amount of the hydrazide 9m on treatment with ammonium acetate in acetic acid.Similar treatment of ketones 2a and 2b afforded only the hydrazides 9a and 9b, respectively.Ketones 2a-n reacted with hydrazine hydrate in acetic acid to give 7H-s-triazolothiadiazines 5a-n.However, ketones 2o-q, with substituents α to the carbonyl group, could not be converted to the corresponding fused-ring systems.Mechanisms for these transformations are proposed.
- Sasaki, Tadashi,Ito, Eikoh,Shimizu, Ikuo
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p. 2757 - 2760
(2007/10/02)
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