Alam Aftab, Elhenawy Ahmed A, Ali Mumtaz, Latif Abdul, Khan Ajmal, Al-Harrasi Ahmed, Ahmad Manzoor
Department of Chemistry, University of Malakand, P.O. Box 18800, Dir Lower, Khyber Pakhtunkhwa, Pakistan.
Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, 11884, Egypt.
Future Med Chem. 2024;16(22):2337-2350. doi: 10.1080/17568919.2024.2401311. Epub 2024 Sep 23.
In light of various biological activities of benzimidazole and azines, this study focuses on reporting novel derivatives of benzimidazole nucleus. Twenty novel azines of benzimidazole were synthesized, characterized and tested for urease inhibitory activity. All these derivatives showed excellent to good inhibition in the range of IC values 14.21 ± 1.87 to 76.11 ± 1.81 μM by comparing with standard thiourea 21.14 ± 0.42 μM. Docking studies were performed for the targeted benzimidazole derivatives to understand the binding mechanics. The results indicated higher binding efficacy compared with the reference inhibitor. This work identifies potential lead candidates for novel urease inhibitors, which with industrial support may be harnessed for the development of new drugs.
鉴于苯并咪唑和嗪类的各种生物活性,本研究着重报道苯并咪唑核的新型衍生物。合成了20种新型苯并咪唑嗪类化合物,对其进行了表征并测试了脲酶抑制活性。通过与标准硫脲(21.14±0.42 μM)比较,所有这些衍生物在IC值14.21±1.87至76.11±1.81 μM范围内表现出优异至良好的抑制作用。对目标苯并咪唑衍生物进行了对接研究,以了解其结合机制。结果表明,与参考抑制剂相比,其结合效力更高。这项工作确定了新型脲酶抑制剂的潜在先导候选物,在工业支持下,这些候选物可用于开发新药。