Drug Res (Stuttg) 2017; 67(09): 515-526
DOI: 10.1055/s-0043-106444
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Synthesis, Characterisation, Molecular Docking, Anti-microbial and Anti-diabetic Screening of Substituted 4-indolylphenyl-6-arylpyrimidine-2-imine Derivatives

Veerasamy Ramya1, Santhirakasu Vembu1, Ganesan Ariharasivakumar2, Manathusamy Gopalakrishnan1
  • 1Department of Chemistry, Annamalai University, Annamalai Nagar, Tamil Nadu, India
  • 2Department of Pharmacology, KMCH College of Pharmacy, Kovai Estate, Tamil Nadu, India
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Publication History

Publication Date:
19 June 2017 (eFirst)

Abstract

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 (11a-g), compound 11a exhibits excellent CDOCKER energy (−11.36 kcal/mol). The entire compounds (11a-g) confirm very good antimicrobial activity towards the tested microorganisms. In the in vitro anti-diabetic studies, compounds (11a, 11c, and 11g) confirm higher alpha-amylase and alpha-glucosidase inhibition activity. In the in vivo anti-diabetic activities, the synthesized compounds (11a-g) (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.

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