439694-28-7Relevant articles and documents
Conformations and receptor activity of desmopressin analogues, which contain γ-turn mimetics or a ψ[CH2O] isostere
Hedenstr?m, Mattias,Yuan, ZhongQing,Brickmann, Kay,Carlsson, Jolanta,Ekholm, Kjell,Johansson, Birgitta,Kreutz, Eva,Nilsson, Anders,Sethson, Ingmar,Kihlberg, Jan
, p. 2501 - 2511 (2002)
Three analogues of the antidiuretic drug desmopressin ([1-desamino,8-D-arginine]vasopressin) have been prepared. In two of these, γ-turn mimetics based on a morpholin-3-one framework have been inserted instead of residues Phe3-Asn5, whereas the third anal
A concise enantioselective synthesis of (R)-selegiline, (S)-benzphetamine and formal synthesis of (R)-sitagliptin via electrophilic azidation of chiral imide enolates
Dey, Soumen,Sudalai, Arumugam
, p. 67 - 72 (2015/02/02)
A concise and high yielding enantioselective synthesis of (R)-selegiline, an anti-Parkinson's drug, (S)-benzphetamine, an anti-obesity agent, and (S)-sitagliptin, an anti-diabetic drug has been described starting from commercially available starting materials employing Evans' electrophilic azidation of chiral imide enolates as a key chiral inducing step, which proceeds in a highly diastereoselective manner (>99%).
Design, synthesis and evaluation of triazole functionalized ring-fused 2-pyridones as antibacterial agents
Bengtsson, Christoffer,Lindgren, Anders E.G.,Uvell, Hanna,Almqvist, Fredrik
body text, p. 637 - 646 (2012/09/08)
Antibacterial resistance is today a worldwide problem and the demand for new classes of antibacterial agents with new mode of action is enormous. In the strive for new antibacterial agents that inhibit pilus assembly, an important virulence factor, routes to introduce triazoles in position 8 and 2 of ring-fused bicyclic 2-pyridones have been developed. This was made via Sonogashira couplings followed by Huisgen 1,3-dipolar cycloadditions. The method development made it possible to introduce a diverse series of substituted triazoles and their antibacterial properties were tested in a whole cell pili-dependent biofilm assay. Most of the twenty four candidates tested showed low to no activity but interestingly three compounds, one 8-substituted and two 2-substituted, showed promising activities with EC50's between 9 and 50 μM.
