Posted by admin on Feb 28, 2019 in |
A series of conjugation of two heterocycles 1, 3, 4-oxadiazole and quinazolone were synthesized and screened for antimicrobial as well as antioxidant activity. Compound4-(4-oxo-2-phenyl-quinazoline-3(4H)-yl)-benzohydrazide 3 on cyclization with different aromatic acids in the presence of phosphoryl chloride (POCl3) give different 1, 3, 4-oxadiazole derivatives. Similarly, compound 3 on reaction with carbon disulphide (CS2) gives substituted oxadiazole thione which on reaction with different halides in the presence of dimethylformamide (DMF) give oxadiazole thiones analogs 6a-6c. Structural assignments of these compounds have been made by elemental analysis, UV, IR, 1H NMR, and mass spectral data. Synthesized analogs were screened for in-vitro growth inhibition activity against different strains of bacteria and fungi and compared with standard drugs ciprofloxacin and fluconazole. Compounds 4e and 4f have good activity against bacteria. All compounds have moderate activity against fungi. These compounds were screened for antioxidant activity by using radical scavenging DPPH assay by using ascorbic acid as a standard drug. Compounds 4e, 6a to 6c have good antioxidant...
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Posted by admin on Jan 31, 2019 in |
The desired target Compounds (4a-e), (5a-e) and (6a-e) were prepared in two steps. Reaction of 3-acetyl-6-bromo-2H-chromen-2-one (1) with 3-(Aryl)-1-phenyl-1H-pyrazole-4-carbaldehydes (2a-e) in presence of aqueous KOH solution and the reaction mixture stirred for 2 hours and then filtered, furnished the desired 6-bromo-3-((E)-3-(3-(Aryl)-1-phenyl- 1H-pyrazole-4-yl) acryloyl)- 2H-chromen-2- ones (3a-e) crystalline solids in 60-70% yield (Scheme-1). Further, compounds (3a-e) reaction with thiourea, urea and hydrazine hydrate in the presence of a base in EtOH yielded the compounds (4a-e), (5a-e) and (6a-e) in 50-85% yield. All the synthesized compounds have been characterized by spectral data’s, and they are screened for anti-microbial activity. Among synthesized compounds 3b, 3c, 3d, 5a, and 5d exhibited good activity against bacterial strains S. aureus, P. aeruginosa, and E. coli, respectively. Whereas other compounds showed poor to moderate activity against all bacterial strains and compounds 3a, 3b, 3d, 4c, 5d, and 5c exhibited good antifungal activity against A. niger, and A. flavus and remaining compounds exhibited moderate antifungal activity. Results were tabulated in Table...
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Posted by admin on Jan 31, 2019 in |
Chytranthus macrobotrys (Sapindaceae) is one of the notable African medicinal plants with traditional history but lack scientific data. This report was aimed to evaluate C. macrobotrys seed (CMS) methanol extract for its phytochemical composition, antimicrobial activity, α-glucosidase, and α-amylase inhibitory activities. Methanolic extract of C. macrobotrys seed was investigated for its chemical composition, antimicrobial activity, α-glucosidase, and α-amylase inhibitory activities. The results revealed the presence of flavonoid (18.61 ± 1.88 mg/100g), phenol (28.71 ± 2.95 mg/100g), tannin (17.29 ± 1.84 mg/100g), terpene (587.07 ± 3.63 mg/100g), sterol (111.54 ± 3.85 mg/100g) and saponin (761.78 ± 1.35 mg/100g). The extract using agar diffusion method showed antimicrobial activity against Staphylococcus aureus, Proteus vulgaris, Pseudomonas aureuginosa, Streptococcus pneumonia, Bacillus cereus, and Micrococcus luteus with a diameter of inhibition zones from 10-20 mm. A weak antimicrobial activity was observed against Escherichia coli and Shigella sp. while no activity was observed against Klebsiella pneumonia and Salmonella typhi. The CMS showed α-glucosidase and α-amylase inhibitory activity at the concentration range of 10-100 µg/ml. The highest...
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Posted by admin on Jan 31, 2019 in |
Swietenia mahagoni (L.) Jacq. belongs to the Meliaceae family and it is native to the West Indies. It was introduced to India in 1975 and now grown in any parts of India. Biological activities of the plant are due to the abundance of phenolic compounds including different terpenoids and limonoids. The plant possesses various secondary metabolites which are responsible for its anti-bacterial, anti-fungal, anti-malarial, anti-diabetic anti-oxidant, anti-ulcer, anti-viral, anti-diarrhoeal, anti-pyretic and anti-inflammatory properties. This antimicrobial activity encouraged to work on identification of phytochemical and antimicrobial investigation of this herbal plant. The seeds and barks of Swietenia mahagoni is subjected to phytochemical screening for secondary metabolites and disk diffusion method for its antimicrobial activity against standard MTCC strains, two bacteria namely Staphylococcus aureus (gram+) (MTCC no. 6908), Escherichia coli (gram-) (MTCC no. 77) and one fungus Aspergillus niger (MTCC No.1344) were used for the study. The qualitative phytochemical tests reveal the presences of phytocompounds including alkaloids, terpenoids, tannins, and glycosides as major active constituents. The seed and bark extracts exhibit positively significant antimicrobial...
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Posted by admin on Nov 30, 2018 in |
Plasmodium falciparum and multidrug resistant bacteria such as Mycobacterium avium, Staphylococcus aureus and Escherichia coli are among the top causes of morbidity and mortality especially in developing countries. These pathogens are responsible for the reported antibiotic resistance incidents globally. Due to the increase in antibiotic resistance worldwide, there is an urgent need for new bioactive compounds. This study aimed at determining the antiplasmodial and antimicrobial activity of secondary metabolites produced by soil actinomycetes. Soil samples were collected from Kavango and Hardap regions and cultured on various media to isolate and identify actinomycetes. Secondary metabolites produced were extracted using different solvents. The antimicrobial activity of different isolated secondary metabolites was determined against M. avium, S. aureus and E. coli. Antiplasmodial activity of four bioactive fractions with potent antibacterial activity was further determined against a chloroquine resistant (D10) P. falciparum strain at various concentrations. Bioactive compounds from two isolates displayed activity against M. avium, whilst another two showed activity against E. coli. None of the secondary metabolites displayed activity against S....
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