Ramya Veerasamy, Vembu Santhirakasu, Ariharasivakumar Ganesan, Gopalakrishnan Manathusamy
Department of Chemistry, Annamalai University, Annamalai Nagar, Tamil Nadu, India.
Department of Pharmacology, KMCH College of Pharmacy, Kovai Estate, Tamil Nadu, India.
Drug Res (Stuttg). 2017 Sep;67(9):515-526. doi: 10.1055/s-0043-106444. Epub 2017 Jun 19.
The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (), compound exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds () confirm very good antimicrobial activity towards the tested microorganisms. In the in vitro anti-diabetic studies, compounds confirm higher alpha-amylase and alpha-glucosidase inhibition activity. In the in vivo anti-diabetic activities, the synthesized compounds (10 mg/kg, p.o.) investigated by the streptozotocin (60 mg/kg, ip) -nicotinamide (120 mg/kg, p.o.) - induced model in adult male albino Wistar rat and these derivatives show considerable fasting blood glucose level when compared to metformin hydrochloride a potent and well-known anti-diabetic drug as a reference.
本研究的目的是合成一系列新型的（E）-2-（4-（1H-吲哚-3-基）-6-对取代苯基嘧啶-2-基）二甲基胍衍生物，起始原料为3-（1H-吲哚-3-基）-1-对取代苯基丙-2-烯-1-酮，并评估它们的分子对接研究、抗菌和抗糖尿病活性。在所有合成的化合物（）中，化合物 表现出优异的CDOCKER能量（-11.36 kcal/mol）。所有化合物（）对测试微生物均表现出非常好的抗菌活性。在体外抗糖尿病研究中，化合物 表现出较高的α-淀粉酶和α-葡萄糖苷酶抑制活性。在体内抗糖尿病活性方面，通过链脲佐菌素（60 mg/kg，腹腔注射）-烟酰胺（120 mg/kg，口服）诱导的成年雄性白化Wistar大鼠模型对合成的化合物 （10 mg/kg，口服）进行了研究，与作为参考的强效且知名的抗糖尿病药物盐酸二甲双胍相比，这些衍生物显示出相当可观的空腹血糖水平。
