59857-86-2Relevant academic research and scientific papers
Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition
Hilton-Proctor, J. P.,Ilyichova, O.,Jennings, I. G.,Johnstone, R. W.,Mountford, S. J.,Scanlon, M. J.,Shortt, J.,Thompson, P. E.,Zheng, Z.
, (2019/11/22)
N-Methylpyrrolidone is a solvent molecule which has been shown to compete with acetyl-lysine-containing peptides for binding to bromodomains. From crystallographic studies, it has also been shown to closely mimic the acetamide binding motif in several bromodomains, but has not yet been directly pursued as a fragment in bromodomain inhibition. In this paper, we report the elaboration of N-methylpyrrolidone as a potential lead in fragment-based drug design. Firstly, N-methylpyrrolidone was functionalised to provide points for chemical elaboration. Then, the moiety was incorporated into analogues of the reported bromodomain inhibitor, Olinone. X-ray crystallography revealed that the modified analogues showed comparable binding affinity and structural mimicry to Olinone in the bromodomain binding site.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00589-00591, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
Pesticide Preparations Containing N-Substituted 2-Pyrrolidone-4-Carboxylic Acid Esters
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Paragraph 0078, (2013/08/28)
Disclosed are pesticide preparations containing a) one or more pesticides and b) one or more N-substituted 2-pyrrolidone-4-carbonic acid esters of formula (1), where R1 and R2 independently represent linear, branched, or cyclic C1-C6 alkyl.
Use Of N-Substituted 2-Pyrrolidone-4-Carboxylic Acid Esters And Solvents
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Paragraph 0056-0057, (2013/08/28)
The invention relates to the use of one or more N-substituted 2-pyrrolidone-4-carbonic acid esters of formula (1), where R1 and R2 independently represent linear, branched, or cyclic C1-C6 alkyl, as (a) solvent(s). Said compounds can be used as solvents in industrial applications, e.g. for the production of varnishes and paints, in chemical syntheses, for cleaning or degreasing, in petrochemical processes, in the electronics and photovoltaic industries, or in pesticide preparations, for example.
Synthesis of pyrrolo[2,3-d][1,2,3]thiadiazole-6-carboxylates via the Hurd-Mori reaction. Investigating the effect of the N-protecting group on the cyclization
Stanetty, Peter,Turner, Martin,Mihovilovic, Marko D.
, p. 367 - 375 (2007/10/03)
A route to methyl pyrrolo[2,3-d][1,2,3]thiadiazole-6-carboxylates as potential plant activators and inducers of systemic acquired resistance (SAR) is reported. A synthetic strategy based on cyclization of the thiadiazole ring system utilizing thionyl chloride via the Hurd-Mori protocol as key step was developed. Success of the ring closure reaction turned out to be highly dependent on the nature of the N-protecting group of the pyrrolidine precursor. While electron donors such as alkyl gave only poor conversion to the required 1,2,3-thiadiazoles, an electron withdrawing substituent such as methyl carbamate gave superior yields.
Dithiolane-Isocyanate Imminium Methylides: A Rapid Stereoselective Entry into γ-Lactams
Fishwick, Colin W. G.,Foster, Richard J.,Carr, Robin E.
, p. 9409 - 9412 (2007/10/02)
Methods have been developed for the generation and trapping of dithiolane-isocyanate imminium methylides which are a new type of azomethine methylide-derived 1,3-dipole.These species add efficiently and stereoselectively to electron deficient olefins yielding novel dithiolane-protected γ-lactams which can be efficiently deprotected to yield the corresponding lactam systems.
