Gupta Deepa, Jain D K
Department of Pharmacy, LBS College of Pharmacy, Jaipur, Rajasthan, India.
Department of Pharmacy, IPS College of Pharmacy, Indore, Madhya Pradesh, India.
J Adv Pharm Technol Res. 2015 Jul-Sep;6(3):141-6. doi: 10.4103/2231-4040.161515.
A large number of 1,2,4-triazole-containing ring system have been incorporated into a wide variety of therapeutically interesting drug candidates including anti-inflammatory, central nervous system stimulants, antianxiety, and antimicrobial agents. To overcome the rapid development of drug resistance, new agents should preferably have chemical characteristics that clearly differ from those of existing agents. Thus led to the design and synthesize the new antimicrobial agents. A novel series of Schiff bases based on of 4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazole-3-thiol scaffold was prepared by heating thiocarbohydrazide and substituted benzoic acid and subsequently, treating with substituted benzaldehydes. Seventeen derivatives were synthesized and were biologically screened for antifungal and antibacterial activity. The newly synthesized derivatives of triazole showed antifungal activity against fungal species, Microsporum gypseum; and antibacterial activity against bacterial species, Staphylococcus aureus. It was observed that none of the compounds tested showed positive results for fungi Candida albicans fungi Aspergillus niger, nor against bacterial strain Escherichia coli. Strong antifungal effects were obtained for the synthesized compounds against M. gypseum and were superior or comparable to standard drug ketoconazole. Similarly, all of the synthesized compounds exhibit strong antibacterial activity against S. aureus and were superior or comparable to standard drug streptomycin. It was found that among the triazole derivatives so synthesized, six of them, showed antifungal activity superior to ketoconazole while one of them, showed antibacterial activity superior to streptomycin. Thus, these can be the potential new molecule as an antimicrobial agent.
大量含1,2,4 - 三唑的环系已被引入到各种各样具有治疗意义的候选药物中,包括抗炎药、中枢神经系统兴奋剂、抗焦虑药和抗菌剂。为了克服耐药性的快速发展,新的药物最好具有与现有药物明显不同的化学特性。因此导致了新型抗菌剂的设计与合成。基于4-(苄叉氨基)-5-苯基-4H-1,2,4 - 三唑-3-硫醇支架制备了一系列新型席夫碱,方法是将硫代碳酰肼与取代苯甲酸加热,随后用取代苯甲醛处理。合成了17种衍生物,并对其抗真菌和抗菌活性进行了生物学筛选。新合成的三唑衍生物对真菌石膏样小孢子菌显示出抗真菌活性,对细菌金黄色葡萄球菌显示出抗菌活性。观察到所测试的化合物对白色念珠菌、黑曲霉以及对大肠杆菌菌株均未显示阳性结果。合成的化合物对石膏样小孢子菌具有很强的抗真菌作用,且优于或与标准药物酮康唑相当。同样,所有合成的化合物对金黄色葡萄球菌均表现出很强的抗菌活性,且优于或与标准药物链霉素相当。发现在如此合成的三唑衍生物中,其中六种显示出优于酮康唑的抗真菌活性,而其中一种显示出优于链霉素的抗菌活性。因此,这些可以成为潜在的新型抗菌剂分子。