1371630-59-9Relevant academic research and scientific papers
1,2,4-Thiadiazoles as promising multifunctional agents for treatment of neurodegenerative diseases
Makhaeva,Proshin,Boltneva,Rudakova,Kovaleva,Serebryakova,Serkov,Bachurin
, p. 1586 - 1591 (2017/03/01)
Detailed studies of properties of new 3-substituted 5-anilino-1,2,4-thiadiazoles containing different substituents at position 3 of the thiadiazole ring were carried out, in particular, their esterase profile and antioxidant properties. It was found that the presence in the molecule of 2-aminopropyl fragment determines an efficient and selective inhibition of butyrylcholinesterase as compared to acetylcholinesterase and carboxylesterase, with radical-scavenging activity being weak. The compounds containing a 2-aminopropenyl fragment possess a high radicalscavenging activity, weakly inhibit cholinesterases, and exhibit anticarboxylesterase activity. A wide spectrum of activity of 3-substituted 5-anilino-1,2,4-thiadiazoles as inhibitors of cholinesterases and highly efficient scavengers of free radicals gives a basis for the optimization of structure and development in this series of original agents for therapy of neurodegenerative diseases.
5-Amino-3-(2-aminopropyl)-1,2,4-thiadiazoles as the basis of hybrid multifunctional compounds
Proshin,Serkov,Petrova,Bachurin
, p. 1148 - 1152 (2015/04/14)
An approach to the synthesis of hybrid multifunctional compounds starting from 1,2,4-thiadiazoles containing an amino group in the side chain was developed.
5-AMINO-1,2,4-THIADIAZOLE DERIVATIVES
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Paragraph 0032-0035; 0042, (2013/09/11)
The present invention relates in general to the field of organic chemistry and, in particular, to novel biologically active compounds of 5-amino[1,2,4]thiadiazole derivatives of the general formula: wherein X is ONO2 or NHR3; R1, R2, and R3 may be the same or different and independently represent hydrogen, alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, as well as R1 together with R2 may represent heterocyclyl (for example, optionally substituted pyrrolidine, piperidine, azepane, piperazine, morpholine, etc.) provided that, when R1 is H, then R2 is other than hydrogen or methyl. 5-Amino-[1,2,4]thiadiazole derivatives are of special interest as drug candidates for prevention and treatment of neurodegenerative diseases, for example, Alzheimer's disease.
