148459-01-2Relevant academic research and scientific papers
1,2,4-oxadiazol derivatives compound and antiviral agent containing the same as an active ingredient
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Paragraph 0187; 0190-0193; 0247; 0250; 0255-0257, (2021/08/24)
1, 2, 4 - Oxadiazole derivative compounds and antiviral agents containing the same as an active ingredient. The compound has antiviral activity without cytotoxicity and has antiviral activity, and thus can be useful as an antiviral agent.
Expanding Synthesizable Space of Disubstituted 1,2,4-Oxadiazoles
Tolmachev, Andrey,Bogolubsky, Andrey V.,Pipko, Sergey E.,Grishchenko, Alexander V.,Ushakov, Dmytro V.,Zhemera, Anton V.,Viniychuk, Oleksandr O.,Konovets, Anzhelika I.,Zaporozhets, Olga A.,Mykhailiuk, Pavel K.,Moroz, Yurii S.
, p. 616 - 624 (2016/10/21)
One-pot synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from carboxylic acids and nitriles was optimized to parallel chemistry. The method was validated on a 141 member library; the desired products were recovered with a high success rate and in moderate yields. Practical application of the approach was demonstrated in the synthesis of bioactive compound pifexole and agonists of free fatty acid receptor 1. A library of 4 948 100 synthesizable drug-like 3,5-disubstituted 1,2,4-oxadiazoles was enumerated based on the method and available validated reagents.
Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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, (2008/06/13)
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Synthesis and Serotonergic Activity of 5-(Oxadiazolyl)tryptamines: Potent Agonists for 5-HT1D Receptors
Street, Leslie J.,Baker, Raymond,Castro, Jose L.,Chambers, Mark S.,Guiblin, Alexander R.,et al.
, p. 1529 - 1538 (2007/10/02)
The synthesis and 5-HT1D receptor activity of a novel series of 5-(oxadiazolyl)tryptamines is described.Modifications of the oxadiazole 3-substituent, length of the linking chain (n), and the amine substituents are explored and reveal a large binding pocket in the 5-HT1D receptor domain.Oxadiazole substituents such as benzyl are accommodated without loss of agonist potency or efficacy.The incorporation of polar functionality on a phenyl or benzyl spacer group results in a 10-fold increase in affinity and functional potency.Optimal 5-HT1D activity is observed when the heterocycle is conjugated with the indole and the benzyl sulfonamides 20t and 20u represent some of the most potent 5-HT1D agonist known.Replacement of O for S in the heterocycle leads to a further increase in potency.Deletion of oxadiazole N-2 does not reduce activity, suggesting the requirements for only one H-bond acceptor in this location.The selectivity of these compounds for 5-HT1D receptors over other serotonergic receptors is discussed.Sulfonamide 20t shows 1000-fold selectivity for 5-HT1D over 5-HT2, 5-HT1C, and 5-HT3 receptors and 10-fold selectivity with respect to 5-HT1A receptors.The functional activity of this series of compounds is studied and demonstrates high 5-HT1D receptor potency and efficacy comparable to that of 5-HT.
