Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors
摘要:
Analogs of the psychotropic phenothiazines were synthesized and examined as antitubercular agents against Mycobacterium tuberculosis H37Rv. The compounds were subsequently counter-screened for binding to the dopaminergic-receptor subtypes D1, D2, D3 and the serotonergic-receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2C. The most active compounds showed MICs from 2 to 4 mu g/mL and had overall reduced binding to the dopamine and serotonin receptors compared to chlorpromazine and trifluoperazine. (C) 2007 Elsevier Ltd. All rights reserved.
Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors
摘要:
Analogs of the psychotropic phenothiazines were synthesized and examined as antitubercular agents against Mycobacterium tuberculosis H37Rv. The compounds were subsequently counter-screened for binding to the dopaminergic-receptor subtypes D1, D2, D3 and the serotonergic-receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2C. The most active compounds showed MICs from 2 to 4 mu g/mL and had overall reduced binding to the dopamine and serotonin receptors compared to chlorpromazine and trifluoperazine. (C) 2007 Elsevier Ltd. All rights reserved.
USE OF BENZENE DERIVATIVES AS CHARGE TRANSFER MEDIATORS
申请人:NOVO NORDISK A/S
公开号:EP0552223A1
公开(公告)日:1993-07-28
[EN] USE OF BENZENE DERIVATIVES AS CHARGE TRANSFER MEDIATORS
申请人:——
公开号:WO1992007263A1
公开(公告)日:1992-04-30
[EN] Benzene derivatives having optionally substituted amino or morpholino in the 1 and 4 position, optionally alkyl in the 2, 3 and 6 position and optionally alkyl or nitro in the 5 position or wherein the 1 and 6 substituents together form a heterocyclic ring, can be used as a charge transfer mediator in a biochemical process involving electron transfer between a redox system and an electrode comprising a paste of electrically conductive particles and a pasting material. [FR] On peut utiliser des dérivés benzéniques possédant un amino ou morpholino facultativement substitué en position 1 et 4, éventuellement un alcoyle en position 2,3, et 6 et éventuellement un alcoyle ou un nitro en position 5 ou dans lesquels les substituants 1 et 6 forment ensemble un noyau hétérocyclique comme médiateur de transfert de charge dans un procédé biochimique comportant le transfert d'électrons entre un système de redox et une électrode comprenant une pâte de particules électriquement conductrices et un matériau d'empâtage.