42956-75-2Relevant academic research and scientific papers
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
Borisevich, Sophia S.,Chernyshov, Vladimir V.,Esaulkova, Iana L.,Popadyuk, Irina I.,Salakhutdinov, Nariman F.,Sinegubova, Ekaterina,Yarovaya, Olga I.,Zarubaev, Vladimir V.
, (2021/12/16)
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
An Efficient Synthesis of 2-Substituted Quinazolin-4(3H)-ones by Using Recyclable Wang Resin Supported Sulfonic Acid Catalyst
Kallam, Srinivasa Reddy,Kalyani, K.
, p. 790 - 796 (2022/03/01)
An efficient synthesis of 2-substituted Quinazolin-4(3H)-ones has been developed from isatoic anhydride with various amidoximes by using a recyclable polymer-supported sulphonic acid catalyst. Excellent functional group compatibility and high yields are the important features of this protocol.
SUBSTITUTED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS
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Page/Page column 264; 267, (2020/08/28)
Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
SO2F2-Mediated one-pot cascade process for transformation of aldehydes (RCHO) to cyanamides (RNHCN)
Ding, Chengrong,Ge, Shuting,Wei, Junjie,Zhang, Guofu,Zhao, Yiyong
, p. 17288 - 17292 (2020/05/18)
A simple, mild and practical cascade process for the direct conversion of aldehydes to cyanamides was developed featuring a wide substrate scope and great functional group tolerability. This method allows for transformations of readily available, inexpensive, and abundant aldehydes to highly valuable cyanamides in a pot, atom, and step-economical manner with a green nitrogen source. This protocol will serve as a robust tool for the installation of the cyanamide moiety in various complicated molecules.
5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein
Malancona, Savina,Mori, Mattia,Fezzardi, Paola,Santoriello, Marisabella,Basta, Andreina,Nibbio, Martina,Kovalenko, Lesia,Speziale, Roberto,Battista, Maria Rosaria,Cellucci, Antonella,Gennari, Nadia,Monteagudo, Edith,Di Marco, Annalise,Giannini, Alessia,Sharma, Rajhans,Pires, Manuel,Real, Eleonore,Zazzi, Maurizio,Dasso Lang, Maria Chiara,De Forni, Davide,Saladini, Francesco,Mely, Yves,Summa, Vincenzo,Harper, Steven,Botta, Maurizio
supporting information, p. 766 - 772 (2020/07/14)
The HIV-1 nucleocapsid (NC) protein is a small basic DNA and RNA binding protein that is absolutely necessary for viral replication and thus represents a target of great interest to develop new anti-HIV agents. Moreover, the highly conserved sequence offers the opportunity to escape the drug resistance (DR) that emerged following the highly active antiretroviral therapy (HAART) treatment. On the basis of our previous research, nordihydroguaiaretic acid 1 acts as a NC inhibitor showing moderate antiviral activity and suboptimal drug-like properties due to the presence of the catechol moieties. A bioisosteric catechol replacement approach led us to identify the 5-dihydroxypyrimidine-6-carboxamide substructure as a privileged scaffold of a new class of HIV-1 NC inhibitors. Hit validation efforts led to the identification of optimized analogs, as represented by compound 28, showing improved NC inhibition and antiviral activity as well as good ADME and PK properties.
SSAO INHIBITOR
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Paragraph 0183-0185; 0197; 0198; 0199, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes
Choung, Wonken,Yang, Deokmo,Kim,Choi, Hyukjoon,Lee, Bo Ram,Park, Min,Jang, Su Min,Lim, Jae Soo,Kim, Woo Sik,Kim, Kyung-Hee,Chin, Jungwook,Jung, Kyungjin,Lee, Geumwoo,Hong,Jang, Tae-ho,Joo, Jeongmin,Hwang, Hayoung,Myung, Jayhyuk,Kim, Seong Heon
, p. 2275 - 2282 (2019/06/27)
As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments
A cascade process for directly converting nitriles (RCN) to cyanamides (RNHCN) via SO2F2-activated Tiemann rearrangement
Zhang, Guofu,Zhao, Yiyong,Ding, Chengrong
supporting information, p. 7684 - 7688 (2019/08/30)
A simple, mild and practical process for the direct conversion of nitriles to cyanamides was newly discovered and exhibited a wide substrate scope as well as great functional group-tolerability (36 examples). In this efficient strategy, the in situ generated amidoximes obtained from the reaction of nitriles with hydroxylamine subsequently underwent Tiemann rearrangement, producing the corresponding cyanamides with great isolated yields under SO2F2. Additionally, the control experiments reportedly shed light on the tentative mechanism involved in the formation and elimination of the key intermediate: a sulfonyl ester.
Copper-catalyzed one-pot synthesis of 1,2,4-triazoles from nitriles and hydroxylamine
Xu, Hao,Ma, Shuang,Xu, Yuanqing,Bian, Longxiang,Ding, Tao,Fang, Xiaomin,Zhang, Wenkai,Ren, Yanrong
supporting information, p. 1789 - 1794 (2015/02/19)
A simple and efficient copper-catalyzed one-pot synthesis of substituted 1,2,4-triazoles through reactions of two nitriles with hydroxylamine has been developed. The protocol uses simple and readily available nitriles and hydroxylamine hydrochloride as th
An Efficient Synthesis of 2-Substituted Quinazolin-4(3 H)-ones Catalyzed by Iron(III) Chloride
Mekala, Ramamohan,Akula, Raghunadh,Kamaraju, Raghavendra Rao,Bannoth, Chandrasekhar Kothapalli,Regati, Sridhar,Sarva, Jayaprakash
supporting information, p. 821 - 826 (2014/04/03)
A simple and highly efficient synthesis of 2-substituted quinazolin-4(3H)-ones by the iron(III) chloride catalyzed reaction of isatoic anhydride with various amidoxime derivatives was developed. Several aryl and alkyl amidoximes were screened to demonstra
