117751-86-7Relevant academic research and scientific papers
RIP1K INHIBITORS
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Page/Page column 61; 62, (2021/10/11)
Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceut
Suzuki-Miyaura cross-coupling reaction of monohalopyridines and L-aspartic acid derivative
Mikagi, Ayame,Tokairin, Dai,Usuki, Toyonobu
, p. 4602 - 4605 (2018/11/25)
Suzuki-Miyaura cross-coupling reaction of halogenated pyridines and a borated L-aspartic acid derivative was conducted. The reactivity of chloro-, bromo-, and iodo-pyridines with substituents at the C2, C3, and C4 positions was investigated. Electron dens
Prodrug forms of N-[(4-deoxy-4-amino-10-methyl)pteroyl]glutamate-γ- [ψP(O)(OH)]-glutarate, a potent inhibitor of folylpoly-γ-glutamate synthetase: Synthesis and hydrolytic stability
Feng, Yan,Coward, James K.
, p. 770 - 788 (2007/10/03)
Ester prodrugs of the phosphinate pseudopeptide N-[(4-deoxy-4-amino-10- methyl)pteroyl]glutamate-γ-[ψP-(O)(OH)]-glutarate (1a) were synthesized. H-phosphinic acids derived from N-Cbz vinyl glycine esters were converted to the desired pseudopeptides by Michael addition to α-methyleneglutarate esters. Pivaloyloxymethyl (POM) ester moieties were incorporated in both the N-terminal and C-terminal fragments prior to formation of either C-P bond, N-Alkylation of the corresponding amides derived from N-(N-methyl)aminobenzoic acid with 2,4-diamino-6-(bromomethyl)pteridine gave the target compounds. POM esters of methotrexate and the corresponding γ-glutamyl conjugate were also synthesized using the same strategy. All prodrugs were evaluated in Chinese hamster ovary cells. Although the pseudopeptide prodrugs were ineffective, prodrugs of methotrexate and the corresponding γ-glutamyl conjugate were equipotent with the parent compounds. Stability of the prodrugs was investigated in both phosphate buffer and cell line medium to provide a rationale for the observed biological data.
The synthesis of diaminopimelic acid containing peptidoglycan fragments using metathesis cross coupling
Chowdhury, Abhijit Roy,Boons, Geert-Jan
, p. 1675 - 1678 (2007/10/03)
Properly protected diaminopimelic acid (DAP), a component of peptidoglycan of Gram-negative bacteria, was prepared by a metathesis cross coupling between properly protected allyl and vinyl glycine derivatives using Grubb's second-generation catalyst follo
Palladium(O) catalysed and copper(I) promoted reactions of the secondary zinc reagent derived from L-threonine
Wilson, Ian,Jackson, Richard F.W.
, p. 2845 - 2850 (2007/10/03)
The preparation of C-3 epimeric secondary zinc reagents from diastereoisomeric iodide using DMF as solvent was discussed and analyzed by NMR methods. Palladium catalysed cross couplings and copper promoted allylations produced protected β-methyl substituted amino acids. It was concluded that the threonine derived zinc reagents were of limited values, but further optimization of copper-promoted reactions make this approach to synthesis of β-methyl substituted α-amino acids more useful.
Glutamyl-γ-boronate inhibitors of bacterial Glu-tRNAGln amidotransferase
Decicco, Carl P.,Nelson, David J.,Luo, Ying,Shen, Li,Horiuchi, Kurumi Y.,Amsler, Karen M.,Foster, Lorie A.,Spitz, Susan M.,Merrill, Jayson J.,Sizemore, Christine F.,Rogers, Kelley C.,Copeland, Robert A.,Harpel, Mark R.
, p. 2561 - 2564 (2007/10/03)
Analogues of glutamyl-γ-boronate (1) were synthesized as mechanism-based inhibitors of bacterial Glu-tRNAGln amidotransferase (Glu-AdT) and were designed to engage a putative catalytic serine nucleophile required for the glutaminase activity of
