90361-99-2Relevant articles and documents
Pyrazinodiazepine derivative and pharmaceutical application thereof
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Paragraph 0031; 0034-0035, (2019/01/24)
The invention relates to a pyrazinodiazepine derivative shown as formula (I) and pharmacologically acceptable salts, isomers, prodrugs and pharmaceutical compositions thereof. The compounds are benzodiazepine receptor antagonist, wherein R can be methyl, ethyl, trifluoroethyl, cyclopropyl, isopropyl and benzyl, and X is hydrogen, chlorine, or 1-tetrahydropyrrole. The invention also discloses preparation of the compounds and application thereof as drugs.
Synthesis and biological evaluation of N-alkyl-3-(alkylamino)-pyrazine-2-carboxamides
Semelkova, Lucia,Konecna, Klara,Paterova, Pavla,Kubicek, Vladimir,Kunes, Jiri,Novakova, Lucie,Marek, Jan,Naesens, Lieve,Pesko, Matus,Kralova, Katarina,Dolezal, Martin,Zitko, Jan
, p. 8687 - 8711 (2016/09/04)
A series of N-alkyl-3-(alkylamino)pyrazine-2-carboxamides and their N-alkyl-3-chloropyrazine-2-carboxamide precursors were prepared. All compounds were characterized by analytical methods and tested for antimicrobial and antiviral activity. The antimycobacterial MIC values against Mycobacterium tuberculosis H37Rv of the most effective compounds, 3-(hexylamino)-, 3-(heptylamino)- and 3-(octylamino)-N-methylpyrazine-2-carboxamides 14-16, was 25 μg/mL. The compounds inhibited photosystem 2 photosynthetic electron transport (PET) in spinach chloroplasts. This activity was strongly connected with the lipophilicity of the compounds. For effective PET inhibition longer alkyl chains in the 3-(alkylamino) substituent in the N-alkyl-3-(alkylamino)pyrazine-2-carboxamide molecule were more favourable than two shorter alkyl chains.
ALPHA 7 NICOTINIC ACETYLCHOLINE ALLOSTERIC MODULATORS, THEIR DERIVATIVES AND USES THEREOF
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, (2013/12/03)
The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.