- A model D - amino acid oxidase inhibitor and its preparation and application
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The invention provides a novel D- amino acid oxidase inhibitor and a preparation and application thereof. In particular, the invention discloses derivatives of quinoxaline-2,3-diketone, which has a novel structure shown in formula A, as well as a preparation method thereof and an application as an inhibitor of D-amino acid oxidase (DAAO). The compound provided by the invention shows excellent effects of analgesia and blocking morphine analgesia tolerance, and has application value for analgesia, treating opiate drug tolerance, and anti-schizophrenia.
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Paragraph 0295; 0296
(2019/02/02)
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- IMIDAZO[4,5-c]PYRIDINE COMPOUNDS AND METHODS OF ANTIVIRAL TREATMENT
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The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.
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Page/Page column 232
(2010/02/12)
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- The synthesis of anti-fixed 3-methyl-3-deaza-2′-deoxyadenosine and other 3h-imidazo[4,5-c]pyridine analogs
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Rotation of a heterocyclic base around a glycosidic bond allows the formation of syn and anti conformations in nucleosides. The syn conformation has been observed primarily in purine-purine mismatches in DNA duplexes. Such mismatches give rise to false positive oligonucleotide hybridization in DNA-based diagnostics. Here we describe the synthesis of an analog of 2′-deoxyadenosine that retains its Watson-Crick functional groups, but cannot form the syn conformation. In this analog, the N3 atom of 2′-deoxyadenosine is replaced by a C-CH3 group to give 7-methyl-1-β-D-deoxyribofuranosyl-1H-imidazo[4,5-c]pyridin-4-ylamine or 3-methyl-3-deaza-2′-deoxyadenosine (3mddA). This modification sterically prevents the syn conformation and 3mddA becomes an anti-fixed nucleoside analog of 2′-deoxyadenosine. The synthesis and conformational analysis of 3mddA and several analogs with an 3H-imidazo[4,5-c]pyridine skeleton are described, as well as their potential applications.
- Irani, Rostem J.,SantaLucia Jr., John
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p. 737 - 751
(2007/10/03)
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