当前位置：
X-MOL 学术
›
J. Heterocycl. Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
An efficient synthesis of designed 4‐thiazolidinone fused pyrimidine derivatives as potent antimicrobial agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-06-23 , DOI: 10.1002/jhet.4070 Janki J. Patel 1 , Mayur I. Morja 1 , Kishor H. Chikhalia 1
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-06-23 , DOI: 10.1002/jhet.4070 Janki J. Patel 1 , Mayur I. Morja 1 , Kishor H. Chikhalia 1
Affiliation
|
A novel series of hybrid 2‐substituted ((pyrimidin‐2‐yl)hydrazinyl)thiazolidin‐4‐one derivatives were synthesized by means of aromatic nucleophilic displacement of chlorine atoms of 2,4,6‐trichloro pyrimidine. Synthesis of some novel 2‐(2‐(6‐morpholino‐4‐substituted(phenyl amino)pyrimidin‐2‐yl)hydrazinyl)thiazol‐4(5H)‐one derivatives have been carried out by the displacement of chlorine atoms on the basis of functionality concept on varying conditions. The synthesized hydrazinyl thiazolidin‐4‐one pyrimidine derivatives were evaluated for their expected antimicrobialactivity; where, the majority of these compounds showed potent antibacterial and antifungal activities against the tested strains of bacteria and fungi. Afforded title analogs were subsequently characterized by elemental analysis, IR, 1H NMR, 13C NMR, Mass spectroscopy. SAR and HOMO‐LUMO studies were also carried out for confirming the structure biological activity. Thus, these studies suggested that hydrazinyl pyrimidine derivatives bearing thiazolidinone moiety are interesting scaffolds for the development of novel antimicrobial agents.
中文翻译：
有效合成设计的4-噻唑烷酮稠合的嘧啶衍生物作为有效的抗菌剂
通过2,4,6-三氯嘧啶的氯原子的芳香亲核置换，合成了一系列新的杂化的2-取代（（嘧啶-2-基）肼基）噻唑烷-4-酮衍生物。一些新的2-（2-（6-吗啉代-4-取代（苯基氨基）嘧啶-2-基）肼基）噻唑-4（5 H）-衍生物的合成是通过在氯原子上置换功能概念在不同条件下的基础。评估了合成的肼基噻唑烷-4-酮嘧啶衍生物的预期抗菌活性；其中，这些化合物中的大多数对被测细菌和真菌菌株显示出有效的抗菌和抗真菌活性。廉价的标题类似物随后通过元素分析IR 1进行表征1 H NMR，13 C NMR，质谱。还进行了SAR和HOMO-LUMO研究，以确认其结构生物学活性。因此，这些研究表明，带有噻唑烷酮部分的肼基嘧啶衍生物是开发新型抗菌剂的有趣支架。
更新日期：2020-06-23
中文翻译：
有效合成设计的4-噻唑烷酮稠合的嘧啶衍生物作为有效的抗菌剂
通过2,4,6-三氯嘧啶的氯原子的芳香亲核置换，合成了一系列新的杂化的2-取代（（嘧啶-2-基）肼基）噻唑烷-4-酮衍生物。一些新的2-（2-（6-吗啉代-4-取代（苯基氨基）嘧啶-2-基）肼基）噻唑-4（5 H）-衍生物的合成是通过在氯原子上置换功能概念在不同条件下的基础。评估了合成的肼基噻唑烷-4-酮嘧啶衍生物的预期抗菌活性；其中，这些化合物中的大多数对被测细菌和真菌菌株显示出有效的抗菌和抗真菌活性。廉价的标题类似物随后通过元素分析IR 1进行表征1 H NMR，13 C NMR，质谱。还进行了SAR和HOMO-LUMO研究，以确认其结构生物学活性。因此，这些研究表明，带有噻唑烷酮部分的肼基嘧啶衍生物是开发新型抗菌剂的有趣支架。
京公网安备 11010802027423号