已经描述了由容易获得的邻甲酰基-芳基酮和芳基/(杂)芳基甲胺有效和碱介导的一锅区域特异性合成结构上多样化的异喹啉和苯并[ h ]异喹啉。通过这种发达的化学方法很容易获得具有挑战性的3-炔基/烯基异喹啉和双异喹啉,它们可进一步用于各种有机转化。操作简便,高原子经济性,广泛的底物范围,官能团耐受性和对大规模合成的适用性是此开发方法的优势。
已经描述了由容易获得的邻甲酰基-芳基酮和芳基/(杂)芳基甲胺有效和碱介导的一锅区域特异性合成结构上多样化的异喹啉和苯并[ h ]异喹啉。通过这种发达的化学方法很容易获得具有挑战性的3-炔基/烯基异喹啉和双异喹啉,它们可进一步用于各种有机转化。操作简便,高原子经济性,广泛的底物范围,官能团耐受性和对大规模合成的适用性是此开发方法的优势。
The present invention relates to broad spectrum β-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) β-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I)
wherein
R
1
is selected from
R
2
is selected from
with certain provisos as herein defined;
in combination with a pharmaceutically acceptable β-lactam antibiotic in an amount which is effective for treating the bacterial infection.
A library of acylhydrazone iron chelators was synthesized and tested for its ability to inhibit the growth of a chloroquine-resistant strain of Plasmodium falciparum. Some of these new compounds are significantly more active than desferrioxamine DFO, the iron chelator in widespread clinical use and also than the most effective chelators. (c) 2005 Elsevier Ltd. All rights reserved.
Synthesis of new acylhydrazones as iron-chelating compounds
作者:John T. Edward、Mario Gauthier、Francis L. Chubb、Premysl Ponka
DOI:10.1021/je00054a044
日期:1988.10
EDWARD, JOHN T.;GAUTHLER, MARIO;CHUBB, FRANCIS L.;PONKA, PREMYSL, J. CHEM. AND ENG. DATA, 33,(1988) N 4, C. 538-540
作者:EDWARD, JOHN T.、GAUTHLER, MARIO、CHUBB, FRANCIS L.、PONKA, PREMYSL
DOI:——
日期:——
Harnessing the reactivity of <i>ortho</i>-formyl-arylketones: base-promoted regiospecific synthesis of functionalized isoquinolines
作者:Pawan K. Mishra、Shalini Verma、Manoj Kumar、Ankit Kumar、Akhilesh K. Verma
DOI:10.1039/c9cc03689j
日期:——
An efficient and base-mediated one-pot regiospecificsynthesis of structurally diversified isoquinolines and benzo[h] isoquinolines from easily accessible ortho-formyl-arylketones and aryl/(het)arylmethanamines has been described. Challenging 3-alkynyl/alkenyl isoquinolines and bis-isoquinolines were easily attained through this developed chemistry, which can be further used for various organic transformations
已经描述了由容易获得的邻甲酰基-芳基酮和芳基/(杂)芳基甲胺有效和碱介导的一锅区域特异性合成结构上多样化的异喹啉和苯并[ h ]异喹啉。通过这种发达的化学方法很容易获得具有挑战性的3-炔基/烯基异喹啉和双异喹啉,它们可进一步用于各种有机转化。操作简便,高原子经济性,广泛的底物范围,官能团耐受性和对大规模合成的适用性是此开发方法的优势。