SYNTHESIS, DOCKING STUDIES AND EVALUATION OF ANTIMICROBIAL AND IN VITRO ANTIPROLIFERATIVE ACTIVITY OF 5H-CHROMENO 4,3-D PYRIMIDIN-2-AMINE DERIVATIVES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 2
Abstract
Objective: Docking studies and synthesis of 4-aryl-5H-chromeno [4,3 -d]pyrimidine-2-amine derivatives to evaluate antimicrobial and in vitro cytotoxicity activity.Methods: Docking studies were performed on Autodock Vina. Computational work was carried out with UCSF Chimera, Argus lab, Marvin beans. Antimicrobial activity was carried out with the agar cup plate method on two gram-positive organisms viz. Bacillus Subtilis and Staphylococcus Aureus and two gram-negative organisms viz. Escherichia Coli and Pseudomonas Aeruginosa. In vitro cytotoxicity was performed on HeLa cell lines with Sulfo Rhodamine B (SRB) assay method.Results: In docking studies compounds CHR 7, CHR 8 and CHR 9 gave highest docking score (binding free energy) and moderate antimicrobial activity against gram positive organisms. All the synthesized compounds showed poor antimicrobial activity against gram negative organisms. In vitro cytotoxicity activity, in terms of growth inhibitory concentration 50 % (GI50) was in the range 37.9 - 57.1 µM. Though synthesised compounds possess moderate GI50, in comparison to standard Adrinamycin the compounds are inactive.Conclusion: A series of 4-aryl-5H-chromeno[4,3 -d]pyrimidine-2-amine derivatives were synthesized and evaluated for antimicrobial and in vitro cytotoxicity studies. The compound CHR 9 was found most active among all the synthesised compounds.
Authors and Affiliations
Rajesh B. Patil, Sanjay D. Sawant
Keywords
Related Articles
- EP ID EP579083
- DOI -
- Views 63
- Downloads 0
OBSERVATIONAL STUDY ON POISON CASES IN A TERTIARY CARE HOSPITAL
Objective: To evaluate the prevalence, pattern, and cause of poisoning. To characterize the poisoning cases admitted in a tertiary care hospital; followed by the outcome and to observe the antidote given for the poison c...
DIGITALISATION AND AUTOMATION IN PHARMACEUTICALS FROM DRUG DISCOVERY TO DRUG ADMINISTRATION
The rapid progress in the pharmaceutical industry is due to the advancement in the digitalization and automation starting from the invention to the administration of the drug. Every advancement in the development of the...
ISOLATION AND CHARACTERIZATION OF POTENTIAL PROBIOTICS FROM FERMENTED RAGI (ELEUSINE CORACANA)
Objective: The aim of this study was to isolate, characterize and identify the potential lactic acid bacteria from fermented ragi millet (Eleusine coracana).Methods: A total of 177 isolates were isolated from the ferment...
PREVALENCE OF MALARIA CASES IN TEA GARDEN AREAS OF LAKHIMPUR DISTRICT, ASSAM
Objective: After observing the increasing trend in numbers of fever cases from Joyhing and Koilamari tea estate, mass fever surveys were conducted to determine the prevalence of malaria cases in the affected areas.Method...
ANTIFUNGAL ACTIVITY OF CYANOTIS AXILLARIS (L.) D. DON EX SWEET AGAINST OPPORTUNISTIC FUNGAL STRAINS
Objective: The main focus of the study was to compare and determine the antifungal activities of different solvent extracts of Cyanotis axillaris.Methods: The dried whole plant of C. axillaris was extracted by sequential...