scholarly journals Studies on Synthesis of Pyrimidine Derivatives and their Pharmacological Evaluation

2007 ◽  
Vol 4 (1) ◽  
pp. 60-66 ◽  
Author(s):  
T. A. Naik ◽  
K. H. Chikhalia
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Insecticidal Activity ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Pyrimidine Derivatives ◽  
Pharmacological Evaluation ◽  
Antitumor Properties ◽  
Morpholine Derivatives ◽  
Anticonvulsant Activities

1,3,4-Oxadiazoles were associated with broad spectrum of biological activities including antituberculosis, anticonvulsant, anti-inflammatory, insecticidal, antifungal, analgesic and antitumor properties. Morpholine derivatives find their wide spectrum of antimicrobial activity and exhibit anthelmintic, bactericidal and insecticidal activity. Pyrimidine derivatives are also reported to possess antibacterial, antimicrobial, antifungal, anticancer and anticonvulsant activities. Encouraged by this observations we decided to synthesised novel pyrimidine derivatives.

scholarly journals COMPARATIVE STUDY ON ANTIMICROBIAL ACTIVITY OF SEAWEEDS

2017 ◽  
Vol 10 (12) ◽  
pp. 384 ◽  
Author(s):  
Sasikala C ◽  
Geetha Ramani D
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Broad Spectrum ◽  
Large Scale ◽  
Biological Activities ◽  
Maximum Activity ◽  
Significant Inhibition ◽  
Drug Formulation ◽  
Active Principle ◽  
Pharmaceutical Industries

Objective: Secondary metabolites from natural resources are a potential source of antimicrobial leads and drugs can exploited to combat antimicrobial resistance in microorganisms. Seaweeds are considered as a valuable source with a broad spectrum of biological activities. Hence, this study was undertaken to screen seaweeds from Mandapam coastal waters, East coast of India, for antimicrobial activity.Methods: Compounds were extracted using methanol from the seaweeds, namely, Halimeda gracilis, Caulerpa serrulata, Sargassum swartzii, Sargassum wightii, Jania rubens, Ulva lactuca, Ulva fasciata, Gracilaria corticata, Stoechospermum marginatum, Caulerpa scalpelliformis, Caulerpa taxifolia, Chaetomorpha crassa, Enteromorpha flexuosa, and Turbinaria ornate. The extracts were screened for their antimicrobial activity against selected bacterial and fungal pathogens.Results: In the present study, S. swartzii, J. rubens, and S. marginatum showed broad spectrum of antibacterial activity against all the test bacterial pathogens. Among these, the maximum activity was exhibited by S. swartzii against Enterococcus faecalis (27.00 ± 0.88) and Streptococcus pyogenes (23.00 ± 0.84), followed by J. rubens against E. faecalis (26.00 ± 0.56) and S. pyogenes (22.00 ± 0.75), and S. marginatum exhibited significant inhibition against Staphylococcus aureus (15.00 ± 0.22) and S. pyogenes (18.00 ± 1.16).Conclusion: These seaweeds with significant antibacterial activity will subjected to phytochemical screening to find out the potential active principle responsible for antimicrobial activity. It is followed by purification and characterization of the compounds for possible application in drug formulation, can take this to large-scale application in pharmaceutical industries.

A multifunctional shape-adaptive and biodegradable hydrogel with hemorrhage control and broad-spectrum antimicrobial activity for wound healing

2020 ◽  
Vol 8 (24) ◽  
pp. 6930-6945
Author(s):  
Lingling Gao ◽  
Jingjie Chen ◽  
Wei Feng ◽  
Qing Song ◽  
Jingjing Huo ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Wound Healing ◽  
Broad Spectrum ◽  
Wound Dressing ◽  
Biological Activities ◽  
Hemorrhage Control ◽  
Injectable Hydrogel ◽  
Oxidized Dextran ◽  
Biodegradable Hydrogel

An injectable hydrogel wound dressing based on an oxidized dextran and ε-poly-l-lysine network has multiple biological activities.

scholarly journals Antimicrobial effect of a cyclic peptide Nostophycin isolated from wastewater cyanobacteria, Nostoc calcicola

2021 ◽  
pp. 94-101
Author(s):  
Vaishali Gupta ◽  
Deepak Vyas
Keyword(s):  
Antimicrobial Activity ◽  
Cyclic Peptide ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Fragmentation Pattern ◽  
Pharmaceutical Application ◽  
Freeze Dried ◽  
Nostoc Calcicola

Different types of peptides are produced by cyanobacteria of the genus Nostoc, which are unique in structure and have a wide spectrum of biological activities. The objective of the study to explore different habitats of organism and study antimicrobial activities to improve their pharmaceutical application and drug like properties by structure modification. A cyclic peptide nostophycin was isolated from Nostoc calcicola (MK506349) through freeze dried lyophilization method. Its structure has been elucidated with FT-IR, 1HNMR, 13CNMR and LC-MS. Glycine, d-glutamine, l-phenylamine, d-isoleucine, l-proline and a novel amino acid Ahoa are constituents of nostophycin. 1HNMR, 13CNMR spectroscopy confirmed the number of protons and carbons, and characteristics peak determined the structure and fragmentation pattern through LCMS.  Nostophycin possess Ahoa instead of Adha which makes it different from microcystin. Nostophycin exhibits antimicrobial activity against E.coli, S. aureus, C. albicens and A. niger. A good antifungal activity (9-52 μg/mL) and moderate  antimicrobial activity (concentration 18-52 μg/mL) were found for nostophycin. In case of already known peptides, these molecules may be further exploited to improve pharmaceutical application and future drug development.

Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones

2019 ◽  
Vol 19 (5) ◽  
pp. 356-375 ◽  
Author(s):  
Christophe Tratrat ◽  
Michelyne Haroun ◽  
Iakovos Xenikakis ◽  
Konstantinos Liaras ◽  
Evangelia Tsolaki ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Bacterial Species ◽  
Antibacterial Properties ◽  
Docking Studies ◽  
In Vivo Evaluation ◽  
Better Than

Background:Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial.Objectives:The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones.Methods:The designed compounds were synthesized using classical methods of organic synthesis. The in vivo evaluation of antimicrobial activity was performed by microdilution method.Results:All compounds have shown antibacterial properties better than that of ampicillin and in many cases better than streptomycin. As far as the antifungal activity is concerned, all compounds possess much higher activity than reference drugs bifonazole and ketoconazole. The most sensitive bacterial species was B. cereus (MIC 6.5-28.4 µmol × 10-2/mL and MBC 14.2-105.0 µmol × 10-2/mL) while the most resistant ones were L. monocytogenes (MIC 21.4-113.6 µmol × 10-2/mL) and E. coli (MIC 10.7- 113.6 µmol × 10-2/mL) and MBC at 42.7-358.6 µmol × 10-2/mL and 21.4-247.2 µmol × 10-2/mL, respectively. All the compounds exhibited antibacterial activity against the three resistant strains, MRSA, P. aeruginosa and E.coli. with MIC and MBC in the range of 0.65-11.00 µmol/mL × 10-2 and 1.30-16.50 µmol/mL × 10-2. Docking studies were performed.Conclusion:Twenty-eight novel thiazole-based chalcones were designed, synthesized and evaluated for antimicrobial activity. The results showed that these derivatives could be lead compounds in search of new potent antimicrobial agents. Docking studies indicated that DNA gyrase, GyrB and MurA inhibition may explain the antibacterial activity.

New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

2018 ◽  
Vol 18 (1) ◽  
pp. 75-87 ◽  
Author(s):  
Michelyne Haroun ◽  
Christophe Tratrat ◽  
Katerina Kositzi ◽  
Evangelia Tsolaki ◽  
Anthi Petrou ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Antimicrobial Properties ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Design Synthesis ◽  
Benzothiazole Derivatives

Background: Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. Objective: The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. Methods: The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. Results: The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. Conclusion: The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.

scholarly journals Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

2016 ◽  
Vol 65 ◽  
pp. 11-26
Author(s):  
Nilesh M. Thumar ◽  
Ankur A. Kaneria ◽  
Milan Vadodaria ◽  
Kartik Ladva
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Pyrimidine Derivatives ◽  
Gram Negative ◽  
H Nmr ◽  
Ketene Dithioacetals ◽  
Convenient Synthesis ◽  
Bacteria And Fungi

A convenient synthesis of substituted Pyrazolo[1,5-a]pyrimidine was carried out by the reaction of different ketene dithioacetals with different aromatic amine in isopropanol in the presence of potassium carbonate. The newly synthesized compound were characterized by1H NMR, IR, Mass and screened for their antimicrobial activity against various strains of bacteria and fungi. From the synthesized different NCEs, compounds 8a, 8d and 8e are broad spectrum drug which can inhibit the growth of gram positive, gram negative bacteria and fungi.

scholarly journals Bioactivity of Origanum oil on Staphylococcus aureus

2008 ◽  
Vol 2 (1) ◽  
pp. 51-56
Author(s):  
Adel Abed Hasony ◽  
Alaa abas Fadhil ◽  
Khulood Al-Samarrae
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Inhibitory Concentration ◽  
Biological Activities ◽  
Antimicrobial Properties ◽  
Inhibition Zone ◽  
Origanum Vulgare ◽  
Origanum Oil ◽  
Oil Extract

The studies revealed that plants oil possesses Antimicrobial properties, the origanum oil organized by a broad spectrum of antimicrobial activity. This oil extract from the Origanum vulgare found in medeternian mountain especially in Turkey. biological activities were studied to determine the effect of origanum oil on Staphylococcus aureus the result revealed that origanum oil were significantly inhibited the growth of the selected bacteria . The study showed that origanum oil has Bactericidal of effect.The inhibition zone (Hz) was determinant by using different concentration from oil as (0.5, 0.25, 0.125)mg/ml . Minimal inhibitory concentration (MIC) of oil was estimated by using different concentration as (1/10, 1/20, 1/30, 1/40, 1/50) µg/mL, the MIC of bacteria was 1/30.

scholarly journals Synthesis, Characterization and Antimicrobial Activity of A Chalcone Derivative

2020 ◽  
pp. 335-343
Keyword(s):  
Antimicrobial Activity ◽  
Organic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Research Papers ◽  
Natural Sources ◽  
New Drug ◽  
Chalcone Derivative ◽  
Anti Inflammatory ◽  
Significant Class

An area of great interest in recent years has been chalcones. Chalcones are the important component of many natural sources and have variety of biological activities. Chalcones which are also known as α,βunsaturated ketones is an significant class of organic compounds and reported to possess a wide spectrum of biological activities such as antibacterial, antifungal, anticancer, anti-inflammatory etc. Abundant research papers have been published and chalcones continue to show promise for new drug investigations. The derivative of chalcones were prepared using Claisen–Schmidt condensation scheme. The structure of the synthesized was confirmed by UV and IR. The compound was also tested for their antimicrobial activity

The Study of Bacillus Subtils Antimicrobial Activity on Some of the Pathological Isolates

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Hussein A Kadhum ◽  
Thualfakar H Hasan2
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Bacterial Growth ◽  
Broad Spectrum ◽  
Inhibitory Activity ◽  
Bacterial Pathogens ◽  
Inhibitory Ability ◽  
Selection Of

The study involved the selection of two isolates from Bacillus subtilis to investigate their inhibitory activity against some bacterial pathogens. B sub-bacteria were found to have a broad spectrum against test bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa. They were about 23-30 mm and less against Klebsiella sp. The sensitivity of some antibodies was tested on the test samples. The results showed that the inhibitory ability of bacterial growth in the test samples using B. subtilis extract was more effective than the antibiotics used.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

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