Naik Kamlesh K, Thangavel Sivakumar, Alam Afroze, Kumar Shailendra
Nandha College of Pharmacy, Perundurai Main Road, Erode, Tamil Nadu-6. India.
School of Pharmaceutical Sciences, Shoolini University, Bajhol, Solan-173229, (Himachal Pradesh). India.
Recent Pat Inflamm Allergy Drug Discov. 2017;11(1):53-63. doi: 10.2174/1872213X11666170119094702.
Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity and side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective.
The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity.
An attempt was made to synthesize a newer series of 3-methyl flavanone derivatives together with the synthesis of a series of 3- hydroxyl flavone analogues. The structures of the test compounds were elucidated and established by UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were subjected for in vitro antimicrobial screening using cup plate methods, followed by the determination of zone of inhibitions.
Two series (each 10) of 3-methyl flavanone and 3-hydroxy flavone derivatives were synthesized. The structures of the test compounds were characterized and established by various spectroscopic methods. The synthesized compounds were screened for in vitro antibacterial and antifungal activity against different strains (3-Gram positive, 3-Gram negative and 2- fungal strains).
Some of the 3- hydroxyl flavones derivatives (1b, 3b, 4b, and 5b) and 3- methyl flavanone derivatives (3a, 1a, 2a and 4a) were found to elicit potent antimicrobial activity. The study revealed that 3-hydroxy flavone derivatives were found to be most active against Gram negative, while 3-methyl flavanone derivatives were active against Gram positive bacteria.
大多数现有的抗菌药物已产生耐药性，其中一些还存在严重的毒性和副作用。因此，需要发现不仅效力强大，而且毒性较小且成本效益高的新型化合物。
本研究的目的是开发新的合成抗菌剂（抗细菌和抗真菌），如3-取代黄酮/黄烷酮衍生物，其应具有显著的效力且毒性低。
尝试合成一系列新的3-甲基黄烷酮衍生物以及一系列3-羟基黄酮类似物。通过紫外光谱、红外光谱、1H-核磁共振、13C-核磁共振和质谱对测试化合物的结构进行了阐明和确定。使用杯碟法对合成的化合物进行体外抗菌筛选，随后测定抑菌圈。
合成了两个系列（各10种）的3-甲基黄烷酮和3-羟基黄酮衍生物。通过各种光谱方法对测试化合物的结构进行了表征和确定。对合成的化合物针对不同菌株（3种革兰氏阳性菌、3种革兰氏阴性菌和2种真菌菌株）进行了体外抗菌和抗真菌活性筛选。
发现一些3-羟基黄酮衍生物（1b、3b、4b和5b）和3-甲基黄烷酮衍生物（3a、1a、2a和4a）具有强大的抗菌活性。研究表明，3-羟基黄酮衍生物对革兰氏阴性菌最具活性，而3-甲基黄烷酮衍生物对革兰氏阳性菌有活性。
