- Novel O-acylated amidoximes and substituted 1,2,4-oxadiazoles synthesised from (+)-ketopinic acid possessing potent virus-inhibiting activity against phylogenetically distinct influenza A viruses
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This article describes the synthesis and antiviral activity evaluation of new substituted 1,2,4-oxadiazoles containing a bicyclic substituent at position 5 of the heterocycle and O-acylated amidoximes as precursors for their synthesis. New compounds were
- Borisevich, Sophia S.,Chernyshov, Vladimir V.,Esaulkova, Iana L.,Popadyuk, Irina I.,Salakhutdinov, Nariman F.,Sinegubova, Ekaterina,Yarovaya, Olga I.,Zarubaev, Vladimir V.
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- MORPHOLINE DERIVATIVES, COMPOSITIONS CONTAINING THEM AND THEIR USE AS THERAPEUTIC AGENTS
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The present invention relates to compounds of formula (I), wherein R. sup.1 and R 4 represent hydrogen, halogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC. sub.1-4 alkyl, C 1-6 alkoxy, C 1-4 alkyl substituted by a hydroxy or C 1-4 alkoxy group, OCF 3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR a, SOR a, SO 2 R a, COR. sup.a, CO 2 R a or CONR a R b, where R. sup.a and R b are each independently hydrogen or C 1-4 alkyl; R. sup.2, R 3 and R 5 represent hydrogen, halogen, C 1-6 alkyl, C 1-4 alkoxy substituted by a C 1-4 alkoxy group, or trifluoromethyl; R 6 represents C 1-6 alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR 7 R 8. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
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