scholarly journals Synthesis and Antimicrobial Activity of Quinazolinone Conjugated Peptides

2010 ◽  
Vol 7 (2) ◽  
pp. 449-456 ◽  
Author(s):  
G. P. Suresha ◽  
K. C. Prakasha ◽  
Wethroe Kapfo ◽  
D. Channe Gowda

Antimicrobial compounds were synthesized by coupling 4-(4-oxo-3,4-dihydroquinazolin-2-yl) butanoic acid with VP, GVP, VGVP and GVGVP peptides. Antimicrobial activities of the synthesized compounds were performed against various bacterial strains by disc diffusion method. The structure activity relationship was evaluated with respect to hydrophobicity, polarity, chain length of peptides and alkyl chain length of quinazolinone. Correlations of analogs with respect to their antimicrobial activity in comparison with conventional drugs and probable mechanism for the activity were discussed.

2017 ◽  
Vol 119 (10) ◽  
pp. 2277-2286 ◽  
Author(s):  
Sireerat Laodheerasiri ◽  
Nirasha Horana Pathirage

Purpose The purpose of this paper is to determine the antimicrobial compounds extracted from various types of soybean materials; raw soybean, soybean flour and roasted soybean. Bacteria growth inhibition was tested in E.coli and S. aureus by disk diffusion method. Efficiency of antimicrobial activities were compared among the extracted solution. Design/methodology/approach Soybean (Glycine max) isoflavones contain the ability to inhibit the growth of many strains of microorganisms. The solid-liquid extraction, ethanol-hexane extraction, was modified to isolate the inhibitory compounds from the three different types of soybean materials. All crude extracts at various concentrations performed under different extracted solutions (75, 50, 25, 12.5, 6.25 and 3.125 percent) were tested with E. coli. and S. aureus to determine the antimicrobial activities and the minimum inhibition concentration (MIC). Disk diffusion method was chosen to study the antimicrobial activity of isoflavones. Findings Soybean flour extract inhibited the growth of E. coli and S. aureus more effective than roasted soybean and raw soybean, respectively. The MIC of inhibitory compounds extracted from soybean flour was 6.25 percent (0.031 mg/ml), roasted soybean was 25 percent (0.125 mg/ml) and raw soybean was 50 percent (0.250 mg/ml). Crude extracts of soybean flour and roasted soybean showed better results than raw soybean. All the three of extracted soybeans inhibited the growth of E. coli better than S. aureus. Originality/value Ethanol-hexane extraction was successfully used to isolate the antimicrobial compounds from raw soybean, soybean flour and roasted soybean. Comparison of antimicrobial activity showed that soybean flour contained the highest inhibition activity.


2021 ◽  
Author(s):  
Julie Piron ◽  
Jessica Pastour ◽  
Niklas Tysklind ◽  
Juliette Smith-Ravin ◽  
Fabienne Priam

AbstractMarine sponges are known for their antimicrobial, antifungal, and cytotoxic activity. In this study, the activity of aqueous and ethanoic extracts of 3 sponges from Martinique were tested on 5 bacterial strains: Bascillus cereus (CIP 783), Echerichia coli (CIP 54127), Pseudomonas aeruginosa (CIP A22), Staphylococcus aureus (CIP 67.8) and Staphylococcus saprophyticus (CIP 76125). The antimicrobial activity of Agelas clathrodes, Desmapsamma anchorata, and Verongula rigida, was demonstrated using the disc diffusion method and by determining the minimum inhibitory concentration and the minimum bactericidal concentration. The ethanoic extract of Agelas clathrodes had an inhibitory activity specifically on Staphylococcus aureus and Staphylococcus saprophyticus. No activity was observed for the other extracts. Further chemical analyses will be carried out in order to identify the active molecules of these sponges.


2019 ◽  
Vol 16 (6) ◽  
pp. 931-938
Author(s):  
Hany M. Mohamed ◽  
Ashraf H.F. Abd El-Wahab

Background: Synthetic azo compounds and their derivatives have been studied extensively due to their biological and pharmacological activities. Pyranopyridines, pyranopyrimidines and tetrazoles derivatives have emerged as a promising and attractive scaffold in the development of potent biological and pharmacological agents. Objectives: To design a series of new benzochromeno(pyridine/pyrimidine/tetrazole) derivatives and evaluate their antimicrobial activity against some bacterial strains (Gram-positive and Gram-negative) and some fungal strains. Materials and Methods: The (E)-7-(4-chlorophenyl)-5-(phenyldiazenyl)-10-thioxo-7,9,10,11-tetrahydro-8Hnaptho[ 1,2-b]pyrano[2,3-d]pyrimidin-8-one (4) was synthesized by the reaction of 4H-naphtho[1,2-b]pyran-3- carbonitrile (3) with carbon disulfide in alcoholic potassium hydroxide solution. Reaction of 3 with sodium azide in DMF and in presence of ammonium chloride afforded 6-(phenyldiazenyl)-3-(1H-tetrazol-5-yl)-4Hbenzo[ h]chromen-2-amine (7) while with malononitrile, thiourea or urea gave chromeno[2,3-b]pyridine-9- carbonitrile (8), chromeno[2,3-d]pyrimidine-10-thione (9) and chromeno[2,3-d]pyrimidin-10-one (10), respectively. The assignment structures were established on the basis of spectral data. Results: In this study, the antimicrobial activity of the synthesized compounds 3-12 was examined for their in vitro antimicrobial activity by using agar diffusion method such as Mueller-Hinton agar medium for bacteria and Sabouraud’s agar medium for fungi. Ampicillin and mycostatine were included in the experiments as reference drugs. Conclusion: A series of new benzochromeno(pyridine/pyrimidine/tetrazole) derivatives were synthesized in this work. All compounds were evaluated in antimicrobial activities.


2016 ◽  
Vol 5 (09) ◽  
pp. 4885 ◽  
Author(s):  
Khushbu Pandey ◽  
Mahendra Singh* ◽  
Bharat Pandey ◽  
Anshulika Upadhyaya ◽  
Kamal K. Pande

The present study was carried out for phytochemical screening of principle bioactive compounds and antimicrobial activity in Elaeocarpus ganitrus Roxb., Phytochemical analysis revealed the presence of saponin, terpenoid, steroid, saponin, flavonoid, tannin and alkaloid. The petroleum, ether, chloroform, methanol, acetone and aqueous extracts were subjected to antimicrobial activity against bacterial strains Staphylococcus aureus, Pseudomonas, E. coli and Bacillus subtilis against anti-fungal strains A.awamori, A.fumigatus, Rhizopus oryzae, Trichoderma viridae and C.oryzae. The antibacterial and antifungal activity was evaluated by disc-diffusion method.


2016 ◽  
Vol 53 ◽  
pp. 57-64
Author(s):  
Radia Mahboub ◽  
Faiza Memmou

We have studied the antimicrobial properties of 6-bromoeugenol and eugenol by three strains:Pseudomonas aeruginosa(S1),Escherichia coli(S2) andStaphylococcus aureus(S3). We have determined the minimum inhibitory concentration (MIC) for a range of concentrations using the disc diffusion method. We note that all samples present an antimicrobial activity toward the tested bacterial strains at different concentrations (1, 0.5 and 0.25 mg/ml). The 6-bromoeugenol gives modest activity with (S1) and (S3). Eugenol reacts positively with thePseudomonas aeruginosa(S1) at all concentrations and with theEscherichiacoli(S2) at 0.5 mg/ml. We remark that thePseudomonas aeruginosa(S1) is the more sensitive strain thanEscherichiacoli(S2) andStaphylococcus aureus(S3). We have estimated the activity coefficient which has confirmed the antimicrobial activity of the different samples. So, 6-bromoeugenol has shown his efficiency as antimicrobial agent.


2020 ◽  
Vol 10 (4) ◽  
pp. 44-48
Author(s):  
Nihed BARGHOUT ◽  
Nada CHEBATA ◽  
Saida MOUMENE ◽  
Seddik KHENNOUF ◽  
Abdelaziz GHARBI ◽  
...  

Polianthes tuberosa L. (Amaryllidaceae) is an ornamental and medicinal plant. Its flowers and bulbs are used traditionally as a diuretic, emetic, against rashes and gonorrhea. The aim of this work was, to evaluate the antioxidant and antimicrobial activities of bulbs and bulbils alkaloid extracts of P. tuberosa. Antiradical effect was assessed against DPPH radical. However, antimicrobial activity was measured through the disc diffusion method against Escherichae coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Staphylococcus aureus resistant to Methicillin (MRSA) and Candida albicans ATCC 90028. The scavenging effect against DPPH showed that the bulbs and bulbils alkaloids extracts exhibited an antiradical effect with IC50 = 0.231±0.017 mg/mL and 0.233±0.093 mg/mL respectively, less than the effect of vitamin C with IC50 = 0.0194±0.0002 mg/mL. Antimicrobial activity results reveal that both alkaloid bulbs extracts at 50 mg/mL did not have any inhibitory effect against the studied strains using the disc diffusion method. According to this work, bulbs and bulbils alkaloid extracts show a moderate antioxidant effect; that could be recommended as a natural antioxidant. Although tuberose bulbs were used traditionally as a soap substitute; bulbs alkaloid extract has no antimicrobial effect. Keywords: Polianthes tuberosa L., bulbs, bulbils, alkaloids, antiradical activity, antimicrobial activity.


2020 ◽  
Vol 12 (3) ◽  
pp. 349-362
Author(s):  
M. G. Rabbani ◽  
M. R. Islam

Present work includes synthesis of five NH-analogues of ciprofloxacin, 2-6 have been prepared to find out their medicinal assessment, for instance, antibacterial, antifungal, and cytotoxicity. The structure of the analogues has been confirmed by FT- IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis. The compounds were screened for their antimicrobial activities by the disc diffusion method. Cytotoxicity was also tested against brine shrimp lethality assay. The antimicrobial activity of the analogues compared with the parent was evaluated against three Gram-positive, five Gram-negative bacterial strains and three fungi. The synthesized compounds showed diverse antimicrobial profile among which derivatives, 2 and 3 possessed enhanced activity in contrast to the ciprofloxacin. Additionally, unlike ciprofloxacin, most of the derivatives were also found to show antifungal activity against Candida albicans. Regarding cytotoxicity, most of the derivatives exhibited better cytotoxic activity than ciprofloxacin.


2019 ◽  
Vol 11 (3) ◽  
pp. 351-363
Author(s):  
M. G. Rabbani ◽  
M. R. Islam

Six novel transition metal complexes of ciprofloxacin-p-nitro benzoyl derived from ciprofloxacin have been synthesized to find out their medicinal evaluation. It has been characterized by different techniques, i.e., UV-Vis, IR, NMR and mass spectrometry together with elemental analysis and molar conductivity. All the compounds were screened for their antimicrobial activities by the disc diffusion method. Cytotoxicity was also made against brine shrimp lethality assay. The antimicrobial activity of the analogues compared with the parent was evaluated against three Gram-positive, seven Gram-negative bacterial strains and three fungi. The synthesized compounds demonstrated a variety of antibacterial profiles among which most of the analogues showed a comparable or better activity compared to the ciprofloxacin. Moreover, unlike ciprofloxacin, most of the derivatives were also found to show antifungal activity. Interestingly, all the derivatives possessed an enhanced activity in comparison to the ciprofloxacin against Candida albicans. Regarding cytotoxicity, most of the derivatives showed to a greater degree cytotoxic agent compared to ciprofloxacin.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Ivanildo Mangueira da Silva ◽  
João da Silva Filho ◽  
Priscila Brandão Gomes da Silva Santiago ◽  
Micalyne Soares do Egito ◽  
Carlos André de Souza ◽  
...  

Antibiotic resistance is considered one of the world's major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL.


Author(s):  
Pavani Bellamkonda ◽  
Ramesh Kumar Koothati ◽  
Aamina Bee ◽  
Abhishree Desai ◽  
G. K. Aarthi ◽  
...  

Objective: Dental caries is an infectious disease in which S. mutans plays a key role. Haphazard and irrational use of antibiotics leads to antibiotic resistance and fatal diarrhoeal diseases in children. Antimicrobial potency of Terminalia chebula and Piper nigrum extracts against several bacterial strains have been documented. The aims of this study were to assess and compare the antimicrobial activities of T. chebula and P. nigrum extracts against S. mutans with Ciprofloxacin as the positive control. Materials and Methods: For this purpose, S. mutans was isolated from plaque samples of people with active caries lesions.  Antimicrobial potency of both T. chebula and P.nigrum were tested using agar well diffusion method. Results: All the tested extracts showed antibacterial activity against S. mutans bacteria. Regarding the two tested herbs extracts, a higher antimicrobial activity was shown by the methanol extract of T. chebula with a mean diameter of inhibition zone was 26.75mm and a minimum inhibitory concentration (MIC) at 25mg /ml concentration followed by acetonic extract. Conclusion: These findings confirm the Antimicrobial potency of T. chebula which can be used as an alternative antibiotic and/or in combination with allopathic antibiotics to prevent the antibiotic resistance.


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