86999-29-3Relevant academic research and scientific papers
Triazolopyridopyrimidine: A new scaffold for dual-target small molecules for Alzheimer's disease therapy
Zribi, Lazhar,Pachòn-Angona, Irene,Bautista-Aguilera, Oscar M.,Diez-Iriepa, Daniel,Marco-Contelles, José,Ismaili, Lhassane,Iriepa, Isabel,Chabchoub, Fakher
, (2020)
Alzheimer's disease (AD) is multifactorial disease characterized by the accumulation of abnormal extracellular deposits of amyloid-beta (Aβ) peptide, and intracellular neurofibrillary tangles (NFTs), along with dramatic neuronal death and decreased levels of choline acetyltransferase. Given the limited therapeutic success of available drugs, it is urgent to explore all the opportunities available to combat this illness. Among them, the discovery of new heterocyclic scaffolds binding different receptors involved in AD should offer structural diversity and new therapeutic solutions. In this context, this work describes new triazolopyridopyrimidine easily prepared in good yields showing anticholinesterase inhibition and strong antioxidant power, particularly the most balanced: 6-amino-5-(4-methoxyphenyl)-2-phenyl-[1,2,4]triazolo[1',5':1,6] pyrido[2,3-d]pyrimidine-4-carbonitrile(3c) with IC50 equal to 1.32 μM against AChE and oxygen radical absorbance capacity (ORAC) value equal to 4.01 Trolox equivalents (TE); thus representing a new and very promising hit-triazolopyridopyrimidine for AD therapy.
Facile one-pot synthesis of new [1,2,4]triazolo[1,5-a]pyridine derivatives by ultrasonic irradiation
Zribi, Lazhar,Zribi, Fathi,Marco-Contelles, José,Chabchoub, Fakher,Ismaili, Lhassane
supporting information, p. 1934 - 1939 (2017/10/13)
Herein, we report an ultrasonic promoted facile and convenient “one-pot” procedure for the synthesis of new [1,2,4]triazolo[1,5-a]pyridine derivatives 3, 4 and 5, using Amberlite IRA-400, in short reaction times and high yields and its comparison with classical reaction conditions. The structures of new compounds were assigned with the help of analytical 1H, 13C NMR, and mass spectral studies.
FUNGICIDAL HETEROCYCLIC COMPOUNDS
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Page/Page column 55, (2010/11/24)
A compound which can specifically or selectively expresses an antifungal activity with a broad spectrum, based on the functional mechanism of 1,6-β-glucan synthesis inhibition, is provided, and an antifungal agent which comprises such a compound, a salt thereof or a solvate thereof is provided. A compound represented by the following formula (I), a salt thereof or a solvate thereof.
Chemistry of 1,3-Oxazine-6-thiones. Ring Transformation
Yokoyama, Masataka,Inazawa, Hiroshi,Shimizu, Tomoji,Kodera, Masahito,Imamoto, Tsuneo
, p. 187 - 194 (2007/10/02)
Two 1,3-oxazine-6-thione derivatives obtained by "S,N-Double Rearrangement" reacted with several nucleophiles to produce 1,3-diazin-6-ones, 6-imino-1,3-oxazines, 1,3,4-triazoles, 1,2,4-oxadiazoles, and 1,3-thiazol-6-ones.Their ring transformations are dis
