SYNTHESIS AND CHARACTERIZATION OF NEW COUMARIN DERIVATIVES CONTAINING VARIOUS MOIETIES WITH ANTIBACTERIAL ACTIVITIES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 8
Abstract
Objective: The purpose of this research is to evaluate the antibacterial activity of different moieties (Schiff bases, chalcones, hydrazones and hydrazinyl thiazole) derivatives, inserted at carbon 8 of 7-hydroxy-4-methyl coumarin, using in vitro, serial broth dilution method.Methods: A series of new coumarin derivatives, including (Schiff bases, chalcones, hydrazones and hydrazinyl thiazole), were prepared from 7-hydroxy-4-methyl coumarin, by insertion of the formyl group, at carbon number 8 using Duff reaction. The structure of the new synthesized derivatives elucidated and confirmed utilizing the corresponding analytical and spectroscopic data; including FT-IR, 13C-NMR, and mass spectroscopy. All new coumarin derivatives have been screened for their preliminary antibacterial activity, by serial broth dilution method against two Gram-positive bacteria (Staphylococcus epidermidis and Staphylococcus hemolyticus) and two Gram-negative bacteria (Escherichia coli and Klebsiella pneumoniae).Results: All the synthesized compounds have been found to exhibit considerable antibacterial activity in vitro. Among all the derivatives, compound (5a), showed the highest rate of inhibition, against (Escherichia coli), while compound (6a), showed the greatest anti-bacterial activity against (Staphylococcus hemolyticus), each with minimum inhibitory concentration of (25µg/ml), and the highest MIC of 200 µg/ml for compound 2, against. Klebsiella pneumoniae.Conclusion: Our results displayed a substantial preliminary antibacterial activity of the new coumarin moieties, especially some hydrazones and chalcones at C8 of the coumarin nucleus, against Gram-positive and a Gram-negative bacteria with distinguished MIC.Â
Authors and Affiliations
Shokhan Jamal Hamid, Ammar A. Razzak Mahmood Kubba
Keywords
Related Articles
- EP ID EP578245
- DOI -
- Views 42
- Downloads 0
THE CORRELATION BETWEEN FRAMINGHAM RISK SCORE AND THE CLINICAL AND BIOCHEMICAL PARAMETERS THAT MEASURE FUNCTIONAL DISABILITY AND DISEASE ACTIVITY IN IRAQI PATIENTS WITH RHEUMATOID ARTHRITIS
Objective: Rheumatoid arthritis (RA) patients have increased morbidity and mortality from premature cardiovascular (CV) disease (CVD). Framingham risk score (FRS) is a simplified coronary prediction tool developed to ena...
BIOLOGICAL AND DOCKING STUDIES OF NOVEL AROYLHYDRAZONES
Objective: Novel aroylhydrazone schiff bases were synthesized and were screened for their biological activities.Methods: Using HCl as a catalyst, all the compounds were synthesized at room temperature and were characteri...
EFFECTS OF CO-TRIMOXAZOLE CO-ADMINISTRATION ON THE PHARMACOKINETICS OF AMODIAQUINE IN HEALTHY VOLUNTEERS
Objectives: Amodiaquine (AQ) is a 4-aminoquinoline antimalarial drug that is rapidly and extensively metabolized mainly by CYP2C8 enzyme to N-desethylamodiaquine (DEAQ). Co-trimoxazole (CTZ) is a combination (sulfamethox...
OPTIMIZATION OF ELECTROPORATION MEDIATED TRANSFORMATION OF LACTOBACILLUS PLANTARUM FOR INDUSTRIAL EXPLOITATION
Objective: The objective of our study was to evaluate different established electrotransformation protocols for their suitability on Lactobacillus plantarum.Methods: We tested strategies of electrical parameters in addit...
PHARMACOGNOSTIC STUDY OF CALLISTEMON CITRINUS L. BARK
Objective: Pharmacognostic study of Callistemon citrinus L. barkMethods: The bark of Callistemon citrinus L. was shade dried and powdered mechanically. The powdered material was used for further Pharmacognostic study. Th...