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.
Fuctionalization of Linear and Angular Phenothiazine and Phenoxazine Ring Systems via Pd(0)/XPhos Mediated Suzuki-Miyaura Cross-coupling Reactions
作者:Efeturi A. Onoabedje、Uchechukwu C. Okoro、David W. Knight、Amitabha Sarkar
DOI:10.1002/jhet.2485
日期:2016.11
Chloro‐substituted phenothiazines and phenoxazines were successfully derivatized with phenylboronic and styrylboronic acids using Suzuki–Miyaura cross‐coupling reaction catalyzed by Pd(0)/XPhos for the first time in good yields. The protocol employed 4 mol% Pd and 7 mol% XPhos with K3PO4 in acetonitrile at 80°C. The reaction condition is compatible with carbonyl and unprotected N–H groups in substrates
首次使用Pd(0)/ XPhos催化的Suzuki-Miyaura交叉偶联反应,成功地用苯基硼酸和苯乙烯基硼酸成功地衍生了氯取代的吩噻嗪和吩恶嗪。该方案在80°C的乙腈中使用4 mol%Pd和7 mol%XPhos和K 3 PO 4。反应条件与底物中的羰基和未保护的NH基团相容。通过组合光谱(UV,IR,1 H和13 C NMR),MS和元素分析数据确定结构归属。
THERMOELECTRIC CONVERSION MATERIAL, AND THERMOELECTRIC CONVERSION ELEMENT PREPARED THEREWITH
申请人:Toyo Ink SC Holdings Co., Ltd.
公开号:EP3902021A1
公开(公告)日:2021-10-27
A thermoelectric conversion material containing an electrically conductive material (A) and an organic compound (B) that are in a relationship satisfying the following formula (1): 0 eV ≤ | (HOMO of the organic compound (B)) - (HOMO of the electrically conductive material (A)) | ≤ 1.64 eV.