Category: 5098-14-6

Tam Huynh Dinh; Kolb, Annie; Gouyette, Catherine; Igolen, Jean published an article in 1975, the title of the article was Synthesis of C-nucleosides. VII. β-D-Ribofuranosyl-2- and -8-adenines.Application In Synthesis of 2-Aminomalononitrile 4-methylbenzenesulfonate And the article contains the following content:

Benzyl (O-benzoyl-5-D-ribofuranosyl)thioformimidate reacted with aminomalodinitrile or with 5-amino-4-cyanoimidazole to yield the two C-nucleoside analogs I and II of adenosine. The β-configuration was determined with NMR and CD spectra. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Application In Synthesis of 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to ribosylthioformimidate aminomalonitrile cycloaddition, imidazole amino ribosylthioformimidate cycloaddition, adenosine carbon nucleoside, Carbohydrates: Nucleosides, Nucleotides and other aspects.Application In Synthesis of 2-Aminomalononitrile 4-methylbenzenesulfonate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Barnathan, Gilles; Huynh Dinh Tam; Kolb, Annie; Igolen, Jean published an article in 1976, the title of the article was Synthesis of C-nucleosides. XI. 2-D-Arabinofuranosylimidazoles and 8-D-arabinofuranosylpurines.Electric Literature of 5098-14-6 And the article contains the following content:

The nucleoside analogs I (R = NH2, SH, R1 = H) were prepared by treating II (R1 = R2 = Bz, R3 = Cl, Br) with Hg(CN)2, cleaving benzoyl groups from II (R1 = R2 = Bz, R3 = CN), treating II (R1 = Bz, R2 = H, R3 = CN) with PhCH2SH, cyclizing II (R1 = Bz, R2 = H, R3 = CH(:NH)SCH2Ph) with H2NCH(CN)2, cyclizing II (R1 = Bz, R2 =H, R3 = 4-cyano-5-amino-2-imidazolyl) with HC(:NH)NH2 or HC(OEt)3 and NaSH, and cleaving the benzoyl groups from I (R1 = Bz). The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Electric Literature of 5098-14-6

The Article related to adenine arabinofuranosyl, mercaptopurine arabinofuranosyl, arabinofuranosyl adenine mercaptopurine, imidazole arabinofuranosyl, Carbohydrates: Nucleosides, Nucleotides and other aspects.Electric Literature of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Taylor, Edward C.; Jacobi, Peter A. published an article in 1976, the title of the article was Pteridines. XXXVII. A total synthesis of L-erythro-biopterin and some related 6-(polyhydroxyalkyl)pterins.Product Details of 5098-14-6 And the article contains the following content:

6-(1-Erythro-1′,2′-dihydroxypropyl)pterin was prepared by cupric acetate oxidation of 5-deoxy-L-arabinose to its osone, transoximation with acetone oxime to the α-ketoaldoxime, condensation with benzyl α-aminocyanoacetate methanesulfate to give II, cyclization with guanidine to biopterin 8-oxide, and deoxygenation with sodium dithionite. The overall yield was 12%. In analogous fashion, 6-(D-arabino-tetrahydroxybutyl)pterin and 6-D-threo-trihydroxypropyl)pterin were prepared from D-glucose and D-xylose, resp. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Product Details of 5098-14-6

The Article related to biopterin synthesis, pterin hydroxyalkyl, arabinose oxidation condensation, neopterin, Carbohydrates: Monosaccharides, Glycals and other aspects.Product Details of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Taylor, Edward C.; Berrier, John V.; Cocuzza, Anthony J.; Kobylecki, Ryszard; McCormack, John J. published an article in 1977, the title of the article was Pteridines. 41. Synthesis and dihydrofolate reductase inhibitory activity of some cycloalka[g]pteridines.COA of Formula: C10H11N3O3S And the article contains the following content:

Eleven homologous 2,4-diaminocycloalka[g]pteridines and derivatives with cycloalkane ring size varying from 5 to 15 were prepared by cyclic condensation of aminomalonitrile tosylate [5098-14-6] with α-oximinocycloalkanones to give aminocyanocycloalka[b]pyrazine oxides followed by deoxygenation and guanidine cyclization, or guanidine cyclization of the pyrazine oxides followed by deoxygenation, or by condensation of 2,4,5,6-tetraaminopyrimidine-HCl [39944-62-2] with a cycloalka-1,2-dione. Inhibition of dihydrofolate reductase [9002-03-3] from Lactobacillus casei, rat liver, L1210, and Trypanosoma cruzi depended on cycloalkane ring size, with 2,4-diaminocyclododeca[g]pteridine (I) [53274-34-3] being most active. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).COA of Formula: C10H11N3O3S

The Article related to dihydrofolate reductase inhibitor aminocycloalkapteridine, cycloalkapteridine dihydrofolate reductase inhibitor, Pharmacodynamics: Structure-Activity and other aspects.COA of Formula: C10H11N3O3S

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Rosowsky, Andre; Chen, Katherine K. N. published an article in 1974, the title of the article was Methotrexate analogs. 4. 7-Methyl derivatives of methotrexate and dichloromethotrexate. New synthesis and some biological studies.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate And the article contains the following content:

Conversion of methotrexate (I) [59-05-2] and 3′,5′-dichloromethotrexate (II) [528-74-5] to their 7-methyl analogs III [35190-25-1] and IV [53729-18-3], resp., to prevent metabolism in vivo to the inactive 7-hydroxy derivatives resulted in marked loss of antileukemic activity in mice and in vitro and loss of inhibitory potency against purified dihydrofolate reductase [9002-03-3] from Lactobacillus casei and L1210-FR8 tumor. The lack of antitumor activity presumably resulted from impaired enzyme binding. III was prepared from 2-amino-5-chloromethyl-3-cyano-6-methylpyrazine 1-oxide [53661-20-4] and diethyl N-(p-N-methylaminobenzoyl)glutamate [2378-95-2] by the method of E. C. Taylor, et al. (1973). The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to methotrexate analog leukemia, dihydrofolate reductase methotrexate analog, Pharmacodynamics: Structure-Activity and other aspects.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Baraldi, Pier Giovanni; Pavani, Maria Giovanna; Nunez, Maria del Carmen; Brigidi, Patrizia; Vitali, Beatrice; Gambari, Roberto; Romagnoli, Romeo published an article in 2001, the title of the article was Antimicrobial and antitumor activity of N-heteroimmine-1,2,3-dithiazoles and their transformation in triazolo-, imidazo-, and pyrazolopyrimidines.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate And the article contains the following content:

The reaction of Appel’s salt with o-aminonitrile heterocyclics gave the corresponding 4-chloro-5-heteroimmine-1,2,3-dithiazoles which were evaluated for their antibacterial, antifungal and antitumor activity. Although all these N-heteroimines were devoid of significant antibacterial activity, they showed significant antifungal activity. Moreover, the same derivatives represent highly versatile intermediates in heterocyclic synthesis, in fact the pyrazoleiminodithiazoles can be converted in one step into 2-cyano derivatives of the corresponding 4-methoxy-pyrazolo[3,4-d]pyrimidines by sodium methoxide in refluxing methanol. This provides a general and attractive route to 4-methoxy-6-cyanopyrazolo[3,4-d]pyrimidines from 1-substituted 5-amino pyrazoles in two simple steps. Finally, the isosteric replacement of the pyrazole ring atoms to give the imidazole[3,4-d]pyrimidine and triazole [4,5-d]pyrimidine ring systems was examined The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to heteroimminedithiazole preparation reaction antifungal antibacterial antitumor, structure activity heteroimminedithiazole antifungal antibacterial antitumor, Pharmacology: Structure-Activity and other aspects.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On July 3, 2003, Hirota, Kosaku; Kazaoka, Kazunori; Sajiki, Hironao published an article.Formula: C10H11N3O3S The title of the article was Synthesis and biological evaluation of 2,8-disubstituted 9-benzyladenines: discovery of 8-mercaptoadenines as potent interferon-inducers. And the article contained the following:

Recently, we have identified 9-benzyl-8-hydroxyadenines bearing an appropriate substituent (a butoxy, propylthio or butylamino group) at the 2-position as potent interferon (IFN)-inducers. Herein we report the design, synthesis, and IFN-inducing activity of 8-substituted 9-benzyladenines possessing such an appropriate substituent at the 2-position. Introduction of the appropriate substituent into the 2-position of the adenine nucleus gave rise to expression of the activity even in 9-benzyladenines bearing no hydroxyl group at the 8-position. An amino group at the 6-position and a hydroxyl or thiol group carrying an acidic proton at the 8-position are required to express excellent IFN-inducing activity. 9-Benzyl-2-butoxy-8-mercaptoadenine indicated the most potent activity with MEC of 0.001 μM. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Formula: C10H11N3O3S

The Article related to benzyladenine mercaptoadenine interferon inducer structure activity relationship, Pharmacology: Structure-Activity and other aspects.Formula: C10H11N3O3S

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 18, 2006, Morwick, Tina; Berry, Angela; Brickwood, Janice; Cardozo, Mario; Catron, Katrina; DeTuri, Molly; Emeigh, Jonathan; Homon, Carol; Hrapchak, Matt; Jacober, Stephen; Jakes, Scott; Kaplita, Paul; Kelly, Terence A.; Ksiazek, John; Liuzzi, Michel; Magolda, Ronald; Mao, Can; Marshall, Daniel; McNeil, Daniel; Prokopowicz, Anthony III; Sarko, Christopher; Scouten, Erika; Sledziona, Cynthia; Sun, Sanxing; Watrous, Jane; Wu, Jiang Ping; Cywin, Charles L. published an article.Computed Properties of 5098-14-6 The title of the article was Evolution of the Thienopyridine Class of Inhibitors of IκB Kinase-β: Part I: Hit-to-Lead Strategies. And the article contained the following:

High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically procured in this way and must undergo a rigorous validation process. This process is described in detail for a collection of screening hits identified as inhibitors of IκB kinase-β (IKKβ), a key regulatory enzyme in the nuclear factor-κB (NF-κB) pathway. From these studies, a promising hit series was selected. Subsequent lead generation activities included the development of a pharmacophore hypothesis and structure-activity relationship (SAR) for the hit series. This led to the exploration of related scaffolds offering addnl. opportunities, and the various structural classes were comparatively evaluated for enzyme inhibition, selectivity, and drug-like properties. A novel lead series of thienopyridines was thereby established, and this series advanced into lead optimization for further development. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Computed Properties of 5098-14-6

The Article related to thienopyridine class inhibitor ikappa b kinase screening preparation structure, Pharmacology: Structure-Activity and other aspects.Computed Properties of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On July 1, 2009, Ronco, Cyril; Sorin, Geoffroy; Nachon, Florian; Foucault, Richard; Jean, Ludovic; Romieu, Anthony; Renard, Pierre-Yves published an article.Reference of 2-Aminomalononitrile 4-methylbenzenesulfonate The title of the article was Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors. And the article contained the following:

A new series of huprines (12-amino-6,7,10,11-tetrahydro-7,11-methanocycloocta[b]quinolines, prepared as huperzine-tacrine hybrids) are prepared and their inhibition of recombinant human acetylcholinesterase (rh-AChE) is reported. We have synthesized two series of huprine analogs; in the first one, the benzene ring of the quinoline moiety has been replaced either by different heterocycles or by Ph groups with electron-withdrawing or electron-donating substituents. In the second series, different short linkers are introduced at the 12-positions of the huprine X and Y skeletons to evaluate the influence of modifications at the 12-position. The compounds are prepared from ethyl- or methyl-substituted bicyclo[3.3.1]non-6-en-3-one by Friedlaender reactions with o-aminocyano aromatic compounds The synthesis of two heterodimers with structures based on huprines has been also reported. Activities ranging from moderate to similar to those of huprines X and Y are obtained, with the most potent analog having a third of the activity of the parent huprines X and Y. Topol. data have been inferred from mol. docking; variation in activity with variation in the linking moieties suggest future structural modifications for activity improvement. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Reference of 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to huprine derivative preparation structure human acetylcholinesterase inhibitor, Pharmacology: Structure-Activity and other aspects.Reference of 2-Aminomalononitrile 4-methylbenzenesulfonate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On January 23, 2014, Schiaffo, Charles E.; Shi, Ce; Xiong, Zhengming; Olin, Michael; Ohlfest, John R.; Aldrich, Courtney C.; Ferguson, David M. published an article.Computed Properties of 5098-14-6 The title of the article was Structure-Activity Relationship Analysis of Imidazoquinolines with Toll-like Receptors 7 and 8 Selectivity and Enhanced Cytokine Induction. And the article contained the following:

Toll-like receptors 7 and 8 (TLRs) have emerged as key targets in the design of small mol. adjuvants and stimulants for use in immunotherapies. This study examines the structure-activity relationship of a series of C2- and N1-substituted C7-methoxy-carbonyl-imidazo-quinolines to gain insight to the structural basis to TLR-7 and -8 selective activity. The anal. is further applied to evaluate the induction of multiple cytokines, including IL-10, IL-12, IL-1β, TNF-α, IFN-α, and IFN-γ, using murine BMDCs and human PBMCs. The results show TLR-7/8 activity is correlated to the C2-alkyl chain length, with peak activity occurring for the Bu (TLR-7) and pentyl (TLR-8) derivatives A similar SAR is identified in the production of IL-1β, IL-12, and IFN-γ, which are shown to depend on both the C2-alkyl chain length and substitution to the N1-position. The compounds were also potent stimulators of IFN-α and IL-10 production but with less pronounced structure-based correlations. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Computed Properties of 5098-14-6

The Article related to preparation structure imidazo quinoline derivative tlr7 tlr8 cytokine, Pharmacology: Structure-Activity and other aspects.Computed Properties of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts