15264-63-8Relevant articles and documents
Design, synthesis and biological evaluation of triazole-oxadiazole conjugates for the management of cognitive dysfunction
Jain, Ankit,Piplani, Poonam
, (2020)
Acetylcholinesterase has been a promising target for the development of putative therapeutics against cognitive decline. The deleterious effect of oxidative stress on the learning and memory paradigms of an individual has also been well documented. In view of this, the present study demonstrates the design, synthesis and pharmacological evaluation of triazole-oxadiazole conjugates. Eighteen novel hybrids (6–23) have been synthesised by employing suitable synthetic procedures and characterized by various spectral and elemental techniques. Further these synthesised compounds were evaluated against behavioural alterations using step down passive avoidance and escape learning protocol at a dose of 0.5 mg/kg with reference to the standard, donepezil. All the synthesised compounds were evaluated for their in vitro acetylcholinesterase (AChE) inhibition at five different concentrations using mice brain homogenate as the source of the enzyme. Biochemical estimation of markers of oxidative stress (lipid peroxidation, superoxide dismutase, glutathione and catalase) has also been carried out to assess the role of synthesised molecules on the oxidative damage induced by scopolamine. The compounds 13, 17 and 23 displayed appreciable activity towards acetylcholinesterase inhibition. These compounds also decreased scopolamine induced oxidative stress, thus serving as promising leads for the amelioration of oxidative stress induced cognitive decline. The molecular docking study performed to predict the binding mode of the compounds also suggested that these compounds bind appreciably to the amino acids present in the active site of the recombinant human acetylcholinesterase (rhAChE). The results indicated that these compounds could be further traversed as inhibitors of AChE and oxidative stress for the treatment of cognitive dysfunction.
Crystal Structure of 2-(Pyridin-4-yl)-5-(Undecylthio)-1,3,4-Oxadiazole
Shen,Wang,Sun,Wu,Tan,Weng,Liu
, p. 1236 - 1240 (2018)
The title compound 2-(pyridin-4-yl)-5-(undecylthio)-1,3,4-oxadiazole (C18H27ON3S) is synthesized, and its structure is confirmed by 1H NMR, MS, elemental analyses and X-ray diffraction. It crystallizes in the monoclinic system, space group P2(1)/c with a = 24.453(17) ?, b = 10.604(7) ?, c = 7.095(5) ?, β = 91.60(2)°, V = 1839(2) ?3, Z = 4, and R = 0.086 for 2295 observed reflections with I > 2σ(I). The preliminary biological test shows that the title compound has good activity against Pythium ultimum with inhibitory to be 77.78%.
ZnCl2 catalyzed efficient synthesis of 1,3,4-oxadiazole and 1,3,4-thiadiazole
Rahman, Md.A.,Karim, Mohammad R.,Arifuzzaman, Md.,Siddiquee, Tasneem A.,Mirza, Aminul H.
, p. 3267 - 3273 (2014)
New methods for the synthesis of 1,3,4-oxadiazole and 1,3,4-thiadiazole have been described. No cyclizations took place in the absence of ZnCl 2. 1,3,4-Thiadiazoles are formed in the presence of ZnCl2 alone, whereas oxadiazoles are produced when a base such as Et3N or KOH was used along with ZnCl2. % Yields are optimized.
Facile conversion of acyldiithiocarbazinate salts to 1,3,4-oxadiazole derivatives under microwave irradiation
Joshi, Sachin,Karnik
, p. 111 - 114 (2002)
Microwave irradiation is found to be especially suitable for salts, as illustrated by the conversion of acyldithocarbazinate salts 1 to 5-substituted-2-mercapto 1,3,4-oxadiazoles 2. This method reduced the reaction time to a few seconds.
Synthesis and tuberculostatic activity of methyl 3-isonicotinoyl-dithiocarbazate and S,S′-dimethyl dithiocarbonate isonicotinoylhydrazone, and their reactions with amines and hydrazines
Foks,Mieczkowska,Janowiec,Zwolska,Andrzejcyk
, p. 810 - 816 (2002)
Methyl 3-isonicotinoyldithiocarbazates and S,S′-dimethyl dithiocarbonate isonicotinoylhydrazone were prepared. Their reactions with primary and secondary amines, diamines, and hydrazines were studied. The newly obtained derivatives did not show tuberculostatic activity in vitro.
HERBICIDAL COMPOUNDS
-
Page/Page column 88-89, (2021/04/10)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.
Pleuromutilin derivative with 1, 3, 4-oxadiazole side chain and preparation and application thereof
-
Paragraph 0055-0056; 0070; 0090; 0094; 0095; 0102, (2021/07/24)
The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with a 1, 3, 4-oxadiazole side chain and preparation and application thereof The pleuromutilin derivative with the 1, 3, 4-oxadiazole side chain is a compound shown in a formula 2 or a pharmaceutically acceptable salt thereof, and a solvent compound, an enantiomer, a diastereoisomer and a tautomer of the compound shown in the formula 2 or the pharmaceutically acceptable salt thereof or a mixture of the solvent compound, the enantiomer, the diastereoisomer and the tautomer in any proportion, including a racemic mixture. The pleuromutilin derivative has good antibacterial activity, is especially suitable for being used as a novel antibacterial agent for systemic system infection of animals or human beings, and has good water solubility.
