Ur Rashid Haroon, Khan Sherwali, Khan Asad, Ahmad Nasir, Shah Tanzeel, Khan Khalid
Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, RS, Brazil.
Department of Chemistry, Rawalpindi Women University, 6th Road Satellite Town, Rawalpindi, Pakistan.
R Soc Open Sci. 2024 Jun 26;11(6):240410. doi: 10.1098/rsos.240410. eCollection 2024 Jun.
Chalcone represents a vital biosynthetic scaffold owing to its numerous therapeutic effects. The present study was intended to synthesize 17 chalcone derivatives (-) by direct coupling of substituted acetophenones and benzaldehyde. The target chalcones were characterized by spectroscopic analyses followed by their antimicrobial, and antileishmanial investigations with reference to standard drugs. The majority of the chalcones displayed good to excellent biological activities. Chalcone (1000 µg ml) exhibited the most potent antibacterial effect with its zone of inhibition values of 30, 33 and 34 mm versus , and respectively. The results also confirmed chalcone to be the most potent versus with the lowest IC value of 0.59 ± 0.12 µg ml. Chalcone (500 µg ml) was noticed to be the most potent antifungal agent with its zone of inhibition being 29 mm against . Computational studies of chalcones and supported the preliminary results. The existence of the amino moiety and bromine atom on ring-A and methoxy moieties on ring-B caused better biological effects of the chalcones. In brief, the investigations reveal that chalcones ( and ) can be employed as building blocks to discover novel antimicrobial agents.
查尔酮因其众多治疗作用而代表着一种重要的生物合成支架。本研究旨在通过取代苯乙酮与苯甲醛的直接偶联来合成17种查尔酮衍生物（-）。通过光谱分析对目标查尔酮进行表征，随后参照标准药物对其进行抗菌和抗利什曼原虫研究。大多数查尔酮表现出良好至优异的生物活性。查尔酮（1000 µg/ml）表现出最有效的抗菌作用，其对[具体菌株1]、[具体菌株2]和[具体菌株3]的抑菌圈直径分别为30、33和34毫米。结果还证实查尔酮对[具体对象]最有效，最低IC值为0.59±0.12 µg/ml。查尔酮（500 µg/ml）被发现是最有效的抗真菌剂，其对[具体真菌]的抑菌圈为29毫米。对查尔酮[具体编号1]和[具体编号2]的计算研究支持了初步结果。A环上氨基部分和溴原子以及B环上甲氧基部分的存在导致查尔酮具有更好的生物学效应。简而言之，研究表明查尔酮（[具体编号1]和[具体编号2]）可作为发现新型抗菌剂的基础材料。
