Multi-substituted imidazolines and method of use thereof

Details Multi-substituted imidazolines and method of use thereof Multi-substituted imidazolines and method of use thereof

C - Chemistry, Metallurgy

07

D

C07D 233/40 (2006.01) C07D 233/22 (2006.01) C07D 233/28 (2006.01) C07D 401/04 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2486836

A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-KB as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ~m/mL.

L'invention concerne une nouvelle classe d'imidazolines utilisées comme acides ou esters à 4 positions présentant une activité anti-inflammatoire et antimicrobienne très puissante. La synthèse de ces imidazolines consiste en une réaction multicomposée applicable à une approche synthétique combinatoire. La combinaison de ces deux caractéristiques essentielles permet d'obtenir un médicament thérapeutique efficace dans le traitement du choc septique ainsi que de nombreuses affections inflammatoires (arthrite et asthme) et infectieuses. L'invention concerne également l'utilisation de cette nouvelle classe d'agents non stéroïdiens en tant qu'agents anti-inflammatoires (pour le traitement de l'asthme, etc.), agents antibactériens et agents antiseptiques. Ces composés sont également utiles dans le traitement des tumeurs (telles que les cancers). Les imidazolines sont des inhibiteurs puissants du facteur de transcription NF-KB et exercent une puissante activité contre les bactéries Gram positives B. subtillus et B. cereus avec des valeurs de CMI de l'ordre de 50 ?m/mL.

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