The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
该发明涉及使用
1,3-双芳基-丙-2-
烯-1-
酮(
香豆素)、
1,3-双芳基-
丙酮-1-
酮(二
氢香豆素)和
1,3-双芳基-丙-2-炔-1-
酮制备用于治疗或预防多种严重疾病的药物组合物,包括i)与炎症细胞因子有害作用相关的疾病,ii)涉及幽门螺旋杆菌感染的疾病,iii)涉及病毒感染的疾病,iv)肿瘤性疾病,v)由微
生物或寄生虫引起的疾病。该发明还涉及新型
香豆素和二
氢香豆素(特别是烷
氧基取代变体),其具有有利的取代模式,对其作为药物物质的效果,以及制备它们的方法,以及包含新型
香豆素的药物组合物。此外,本发明涉及一种用于分离利什曼氏弓形虫
富马酸还原酶的方法,以及用于选择上述目的的有效化合物的Q
SAR方法。