Antiarythmiques apparentés au procaïnamide III: N1-acetyl N2-(dialkylaminoalkyl)-4-alcoxybenzamidines
摘要:
Acetylation of the N-[-2-(diethylamino)-ethyl]-4-ethoxybenzamidine improves very much the antiarrhythmic activity of this amidine. The authors describe the preparation, structure and properties of this amidine as well as some pharmacological studies.
[EN] NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS<br/>[FR] NOUVEAUX GLYCOPEPTIDES SEMI-SYNTHÉTIQUES EN TANT QU'AGENTS ANTIBACTÉRIENS
申请人:LEAD THERAPEUTICS INC
公开号:WO2010048340A2
公开(公告)日:2010-04-29
Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid -7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.