Synthesis, Characterization and in silico evaluations of Diethyl-3-Methyl-5-(6-Methyl-2-Oxo-4-Phenyl- 1, 2, 3, 4-Tetrahydropyrimidine-5-Carboxamido) Thiophene-2, 4- Dicarboxylate Analogues as Anti-Proliferative and Anti-Microbial Agents
Journal Title: World Journal of Pharmaceutical Sciences - Year 2016, Vol 4, Issue 9
Abstract
With an aim to develop potent anticancer agents, a series of diethyl-3-methyl-5-(6-methyl-2-oxo -4-phenyl-1, 2, 3, 4-tetrahydropyrimidine-5-carboxamido) thiophene-2, 4-dicarboxylate analogues (KM1-9) have been synthesized by conventional method and characterized by IR, Mass, NMR and elemental analysis. In silico studies have been done for all molecules (KM1-9) on Human topoisomerase IIbeta (PDB Id: 3QX3). The compounds were tested for in vitro antiproliferative activity on VERO and 786-O cell lines. The compound KM5 showed moderate activity on both cell lines. In vitro antimicrobial activity was checked against Bacillus Subtilis (BS), Staphylococcus Aurous (SA), Pseudomonas Aeruginosa (PA), Escherichia Coli (EC) and Candida Albicans (CA) by well diffusion method. The compounds KM3 and KM8 were found to have highest zone of inhibition against BS, SA, PA and EC. The Molecules KM8 and KM9 exhibited comparable activity against PA. The antifungal activity of all the analogous indicated weak activity against CA.
Authors and Affiliations
Dr. Hiren V. Doshi
Keywords
Related Articles
- EP ID EP201986
- DOI -
- Views 68
- Downloads 0
Mouth Dissolving Tablets- A Review
Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded to be safe, economical, easy to form and the most important is the patient compliance. Other various dosage forms are also...
The correlation between statin usage and incidence of depression in a tertiary care hospital
Background: Investigators found that low serum cholesterol levels are an inconsistent possible biological marker for the manifestation of depression and/or suicidal ideation in some individuals. The results of many studi...
Formulation and stability study of lipid-based formulations for oral administration of poorly water-soluble drug
Rousuvastatin calcium (ROS) is a model of poorly water-soluble drug. The objective of the study was to increase the dissolution rate and stability of ROS through formulation of basic tablets, contain nanoemulsion of the...
Silver nanoparticles, Antimicrobial activity, Delonix regia, Antioxidant activity
Karpur has been used by ancient period for promotion of pain healing. A vast drug review shows that this drug also posses analgesic activity. The analgesic effect of this plant when used in anal fissure may be of great v...
An observatory study about Diabetic Screening and Counseling OPD
Diabetes is one of the most costly and burdensome chronic diseases of contempraroy era. Individuals with type 2 diabetes are also at a significantly higher risk for coronary heart disease, peripheral vascular disease, hy...