4342-08-9Relevant academic research and scientific papers
Cytoprotective activities of kinetin purine isosteres
Maková, Barbara,Mik, Václav,Li?ková, Barbora,Gonzalez, Gabriel,Vítek, Dominik,Medvedíková, Martina,Monfort, Beata,Ru?ilová, Veronika,Kadlecová, Alena,Khirsariya, Prashant,Gándara Barreiro, Zoila,Havlí?ek, Libor,Zatloukal, Marek,Soural, Miroslav,Paruch, Kamil,D'Autréaux, Benoit,Hajdúch, Marián,Strnad, Miroslav,Voller, Ji?í
, (2021/01/28)
Kinetin (N6-furfuryladenine), a plant growth substance of the cytokinin family, has been shown to modulate aging and various age-related conditions in animal models. Here we report the synthesis of kinetin isosteres with the purine ring replace
Discovery of novel triazole compounds as selective IL-1β releasement inhibitors
Chen, Leyuan,Gou, Wenfeng,Hou, Wenbin,Li, Yiliang,Mu, Ruixu,Wei, Huiqiang,Ye, Caiying,Yu, Jingcheng,Zhou, Yongting,Zhu, Lei
supporting information, (2021/10/27)
Inflammation and immunity are closely related to the occurrence and development of a variety of immune diseases. Although IL-1β has been identified as a key cytokine in many immune diseases, safe and specific small molecular IL-1β releasement inhibitors a
Water/Alkali-Catalyzed Reactions of Azides with 2-Cyanothioacetamides. Eco-Friendly Synthesis of Monocyclic and Bicyclic 1,2,3-Thiadiazole-4-carbimidamides and 5-Amino-1,2,3-triazole-4-carbothioamides
Filimonov, Valeriy O.,Dianova, Lidia N.,Beryozkina, Tetyana V.,Mazur, Dmitrii,Beliaev, Nikolai A.,Volkova, Natalia N.,Ilkin, Vladimir G.,Dehaen, Wim,Lebedev, Albert T.,Bakulev, Vasiliy A.
, p. 13430 - 13446 (2019/10/16)
The reactions of thioamides with azides in water were studied. It was reliably shown that the reaction of 2-cyanothioacetamides 1 with various types of azides 2 in water in the presence of alkali presents an efficient, general, one-step, atom-economic, and eco-friendly method for the synthesis of 1,2,3-thiadiazol-4-carbimidamides 5 and 1,2,3-triazole-4-carbothioamides 4. This method can be extended to the one-pot reaction of sulfonyl chlorides and 6-chloropyrimidines 2′o with sodium azide, leading to final products in higher yields, that is, avoiding the isolation of unsafe sulfonyl azides. The method was furthermore applied to the reaction of N,N′-bis-(2-cyanothiocarbonyl)pyrazine 1h with sulfonyl azides to afford bicyclic 1,2,3-thiadiazoles 8 and 1,2,3-triazoles 9 connected via a 1,1′-piperazinyl linker. 2-Cyanothioacetamides 1 were also shown to react with aromatic azides in water in the presence of alkali to afford 1-aryl-5-amino-1,2,3-triazole-4-carbothioamides 11. In contrast to aromatic azides and similarly to sulfonyl azides, 6-azidopyrimidine-2,4-diones 2o-q react with cyanothioacetamides to form N-pyrimidin-6-yl-5-dialkylamino-1,2,3-thiadiazole-4-N-l-carbimidamides 12. A mechanism was proposed to rationalize the role of water in changing the reactivity of azides toward 2-cyanothioacetamides.
NEW TRPA1 ANTAGONISTS
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Page/Page column 37; 38, (2017/05/02)
The present invention relates to bicyclic heterocyclic derivatives of Forrmula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
NEW TRPA1 ANTAGONISTS
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Page/Page column 58; 59, (2017/08/01)
The present invention relates to compounds of Formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
IRAK INHIBITORS AND USES THEREOF
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Paragraph 00349, (2017/01/26)
The present invention provides compounds, compositions thereof, and methods of using the same for inhibiting one or more interleukin-1 receptor-associated kinases ("IRAK").
Energetic derivatives of 5-(5-amino-2H-1,2,3-triazol-4-yl)-1H-tetrazole
Izsák, Dániel,Klap?tke, Thomas M.,Pflüger, Carolin
, p. 17054 - 17063 (2015/10/12)
This study presents the preparation of the novel nitrogen-rich compound 5-(5-amino-2H-1,2,3-triazol-4-yl)-1H-tetrazole (5) from commercially available chemicals in a five step synthesis. The more energetic derivatives with azido (6) and nitro (7) groups, as well as a diazene bridge (8) were also successfully prepared. The energetic compounds were comprehensively characterized by various means, including vibrational (IR, Raman) and multinuclear (1H, 13C, 14N, 15N) NMR spectroscopy, mass spectrometry and differential thermal analysis. The sensitivities towards important outer stimuli (impact, friction, electrostatic discharge) were determined according to BAM standards. The enthalpies of formation were calculated on the CBS-4M level of theory, revealing highly endothermic values, and were utilized to calculate the detonation parameters using EPXLO5 (6.02).
NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES
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Paragraph 0908; 0909; 0910, (2013/05/21)
The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
[1, 2, 3] TRIAZOLO [4, 5 -D] PYRIMIDINE DERIVATIVES AS AGONISTS OF THE CANNABINOID RECEPTOR 2
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Page/Page column 163, (2013/05/23)
The invention relates to a compound of formula (I), wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament as agonists of the cannabinoid receptor 2.
8-Azapurines as new inhibitors of cyclin-dependent kinases
Havlicek, Libor,Fuksova, Kveta,Krystof, Vladimir,Orsag, Martin,Vojtesek, Borivoj,Strnad, Miroslav
, p. 5399 - 5407 (2007/10/03)
Purine inhibitors of cyclin-dependent kinases (CDK) seem to be a potential anticancer drug candidate as one of the first representatives, roscovitine, is passing Phase II clinical trials for cancer and glomerulonephritis. In this article, we describe a no
