Kethireddy Shashikala, Eppakayala Laxminarayana, Maringanti Thirumala Chary
Geethanjali College of Engineering and Technology, Keesara, Rangareddy, 501301 Telangana India ; Mahatma Gandhi Institute of Technology, Gandipet, Hyderabad, 500 075 Telangana India.
Mahatma Gandhi Institute of Technology, Gandipet, Hyderabad, 500 075 Telangana India.
Chem Cent J. 2015 Sep 24;9(1):51. doi: 10.1186/s13065-015-0121-4. eCollection 2015 Dec.
The intensely increasing multi-drug resistant microbial infections have encouraged the search for new antimicrobial agents. Hydrazone derivatives are known to exhibit a wide variety of biological activities including anti-microbial. In heterocyclic moiety, imidazo[1,2-a]pyrimidines are the subject of immense interest for their antimicrobial activity and also for their analgesic, antipyretic and anti-inflammatory properties.
Condensation of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide with aromatic aldehydes in ethanol at reflux led to the generation of hydrazone derivatives in 80-92% yield. The synthesis of carbohydrazide was accomplished in six steps from commercially available 2-amino pyrimidine. The structures of the synthesized compounds were confirmed by H, C NMR, Mass and IR spectral data. All the synthesized hydrazone derivatives were tested in vitro for their antibacterial activity. Compounds , and exhibited excellent antibacterial activity with zone of inhibition 30-33 mm against (Gram negative bacteria) and (Gram positive bacteria). These compounds also exhibited excellent antibacterial activity with zone of inhibition 22-25 mm against (Gram negative bacteria) and (Gram positive bacteria).
Synthesized and recorded antibacterial activity of some new 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine-hydrazone derivatives.Graphical abstract:Synthesis of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide derivatives.
多重耐药微生物感染的急剧增加促使人们寻找新的抗菌剂。已知腙衍生物具有多种生物活性，包括抗菌活性。在杂环部分，咪唑并[1,2-a]嘧啶因其抗菌活性以及镇痛、解热和抗炎特性而备受关注。
5,6,7,8-四氢咪唑并[1,2-a]嘧啶-2-碳酰肼与芳香醛在乙醇中回流缩合，以80-92%的产率生成腙衍生物。碳酰肼的合成从市售的2-氨基嘧啶开始，分六步完成。通过氢谱、碳谱、质谱和红外光谱数据确认了合成化合物的结构。所有合成的腙衍生物均进行了体外抗菌活性测试。化合物 、 和 表现出优异的抗菌活性，对 （革兰氏阴性菌）和 （革兰氏阳性菌）的抑菌圈为30-33毫米。这些化合物对 （革兰氏阴性菌）和 （革兰氏阳性菌）也表现出优异的抗菌活性，抑菌圈为22-25毫米。
合成并记录了一些新型5,6,7,8-四氢-咪唑并[1,2-a]嘧啶-腙衍生物的抗菌活性。
5,6,7,8-四氢咪唑并[1,2-a]嘧啶-2-碳酰肼衍生物的合成。
