Yu Haitao, Rehman Najeeb Ur, Ali Mumtaz, Alam Aftab, Latif Abdul, Shahab Nazish, Amir Khan Irfan, Jabbar Shah Abdul, Khan Momin, Al-Ghafri Ahmed, Al-Harrasi Ahmed, Ahmad Manzoor
College of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024, China.
Department of Chemistry, University of Malakand, Chakdara 18800, Pakistan.
Antibiotics (Basel). 2022 Nov 7;11(11):1568. doi: 10.3390/antibiotics11111568.
Polyhydroquinoline (PHQ) are the unsymmetrical Hantzsch derivatives of 1,4-dihydropyridines with several biological applications. In this work, twenty-five (-) new Schiff's base derivatives of polyhydroquinoline hydrazide were synthesized in excellent to good yields by a multi-component reaction. The structures of the synthesized products (-) were deduced with the help of spectroscopic techniques, such as H-, C -NMR, and HR-ESI-MS. The synthesized products (-) were tested for their antibacterial and in vitro calcium -channel-blocking (CCB) potentials using the agar-well diffusion method, and isolated rat aortic ring preparations, respectively. Among the series, sixteen compounds were found to inhibit the growth of and . Among them, compound was observed to be the most potent one at a dose 2 µg/mL, with an 18 mm zone of inhibition against both bacteria when it was compared with the standard drug amoxicillin. Eight compounds showed CCB activity of variable potency; in particular, compound was more potent, with an EC value of 0.7 (0.3-1.1) µg/mL, indicating their CCB effect.
聚氢喹啉（PHQ）是1,4 - 二氢吡啶的不对称汉茨希衍生物，具有多种生物学应用。在本工作中，通过多组分反应以优异至良好的产率合成了25种新型聚氢喹啉酰肼席夫碱衍生物。借助光谱技术，如氢谱、碳谱、氮谱和高分辨电喷雾电离质谱，推导了合成产物的结构。分别使用琼脂孔扩散法和分离的大鼠主动脉环制剂对合成产物进行了抗菌和体外钙通道阻滞（CCB）潜力测试。在该系列中，发现16种化合物可抑制[具体细菌名称未给出]和[具体细菌名称未给出]的生长。其中，化合物[具体化合物编号未给出]在剂量为2 µg/mL时被观察到是最有效的，与标准药物阿莫西林相比，对两种细菌的抑菌圈直径均为18 mm。8种化合物表现出不同程度的CCB活性；特别是化合物[具体化合物编号未给出]更有效，其半数有效浓度（EC）值为0.7（0.3 - 1.1）µg/mL，表明了它们的CCB效应。
