Gupta Deepa, Jain D K
Department is Pharmacy, L.B.S. College of Pharmacy, Jaipur, Rajasthan, India.
Department is Pharmacy, I.P.S. College of Pharmacy, Indore, Madhya Pradesh, India.
J Adv Pharm Technol Res. 2015 Jul-Sep;6(3):114-7. doi: 10.4103/2231-4040.161507.
Much research has been carried out with the aim to discover the therapeutic values of chalcone derivatives. Chalcones possess wide range of pharmacological activity such as antibacterial, antimalarial, antiprotozoal, antitubercular, anticancer, and antifungal agents etc. The presence of reactive α,β-unsaturated keto group in chalcones is found to be responsible for their biological activity. The rapid developments of resistance to antifungal agents, led to design, and synthesize the new antifungal agents. The derivatives of chalcones were prepared using Claisen-Schmidt condensation scheme with appropriate tetralone and aldehyde derivatives. Ten derivatives were synthesized and were biologically screened for antifungal activity. The newly synthesized derivatives of chalcone showed antifungal activity against fungal species, Microsporum gypseum. The results so obtained were superior or comparable to ketoconazole. It was observed that none of the compounds tested showed positive results for fungi Candida albicans nor against fungi Aspergillus niger. Chalcone derivatives showed inhibitory effect against M. gypseum species of fungus. It was found that among the chalcone derivatives so synthesized, two of them, that is, 4-chloro derivative, and unsubstituted derivative of chalcone showed antifungal activity superior to ketoconazole. Thus, these can be the potential new molecule as antifungal agent.
为了发现查尔酮衍生物的治疗价值,人们进行了大量研究。查尔酮具有广泛的药理活性,如抗菌、抗疟疾、抗原虫、抗结核、抗癌和抗真菌等。人们发现查尔酮中活性α,β-不饱和酮基团的存在是其生物活性的原因。由于对抗真菌药物的耐药性迅速发展,促使人们设计并合成新的抗真菌药物。查尔酮衍生物是采用克莱森-施密特缩合方案,用适当的四氢萘酮和醛衍生物制备的。合成了十种衍生物,并对其进行了抗真菌活性的生物学筛选。新合成的查尔酮衍生物对石膏样小孢子菌显示出抗真菌活性。所获得的结果优于酮康唑或与之相当。据观察,所测试的化合物对白色念珠菌和黑曲霉均未显示阳性结果。查尔酮衍生物对石膏样小孢子菌具有抑制作用。发现在如此合成的查尔酮衍生物中,其中两种,即4-氯衍生物和未取代的查尔酮衍生物显示出优于酮康唑的抗真菌活性。因此,这些可能是潜在的新型抗真菌分子。