Department of Pharmaceutical Chemistry, Vignan Pharmacy College, Jawaharlal Nehru Technological University, Vadlamudi 522 213, India.
Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, Ajman University, Ajman PO Box 346, UAE.
Molecules. 2020 Jul 13;25(14):3188. doi: 10.3390/molecules25143188.
Infectious diseases caused by fungi and mycobacteria pose an important problem for humankind. Similarly, cancer is one of the leading causes of death globally. Therefore, there is an urgent need for the development of novel agents to combat the deadly problems of cancer, tuberculosis, and also fungal infections. Hence, in the present study, we designed, synthesized, and characterized 30 compounds including 15 chalcones (-) and 15 dihydropyrazoles (-) containing dichlorophenyl moiety and also screened these compounds for their antifungal, antitubercular, and antiproliferative activities. Among these compounds, the dihydropyrazoles showed excellent antifungal and antitubercular activities whereas the chalcones exhibited promising antiproliferative activity. Among the dihydropyrazoles, compound containing 2-thienyl moiety showed promising antifungal activity (MIC 5.35 µM), whereas compounds and containing 2,4-difluorophenyl and 4-trifluoromethyl scaffolds revealed significant antitubercular activity with the MICs of 3.96 and 3.67 µM, respectively. Compound containing 2-thienyl moiety in the chalcone series showed the highest anti-proliferative activity with an IC value of 17 ± 1 µM. The most active compounds identified through this study could be considered as starting points in the development of drugs with potential antifungal, antitubercular, and antiproliferative activities.
由真菌和分枝杆菌引起的传染病对人类构成了重要问题。同样，癌症是全球主要的死亡原因之一。因此，迫切需要开发新的药物来对抗癌症、结核病和真菌感染等致命问题。因此，在本研究中，我们设计、合成和表征了 30 种化合物，包括 15 种含二氯苯基部分的查尔酮（-）和 15 种二氢吡唑（-），并筛选了这些化合物的抗真菌、抗结核和抗增殖活性。在这些化合物中，二氢吡唑类化合物表现出优异的抗真菌和抗结核活性，而查尔酮类化合物表现出有希望的抗增殖活性。在二氢吡唑类化合物中，含有噻吩基部分的化合物 表现出有希望的抗真菌活性（MIC 5.35 µM），而含有 2,4-二氟苯基和 4-三氟甲基支架的化合物 和 则显示出显著的抗结核活性，MIC 分别为 3.96 和 3.67 µM。在查尔酮系列中含有噻吩基部分的化合物 表现出最高的抗增殖活性，IC 值为 17 ± 1 µM。通过这项研究确定的最有效化合物可以被认为是开发具有潜在抗真菌、抗结核和抗增殖活性的药物的起点。
