Synthesis and Antibacterial Study of Novel Piperazine Linked Methylene-bis-Coumarins

2019 ◽  
Vol 4 (2) ◽  
pp. 101-108
Author(s):  
A. Nagaraj ◽  
S. Srinivas ◽  
P. Ramesh Naik ◽  
R. Neelofer
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Good Activity ◽  
Bacterial Strains ◽  
Antibacterial Study ◽  
Piperazine Ring ◽  
Evaluation Data ◽  
Antibacterial Evaluation ◽  
Potent Inhibitory Activity

A series of new 6-(2-oxo-3-[(4-arylpiperazino)carbonyl]-2H-6-chromenyl-methyl)-3-[(4- arylpiperazino)carbonyl]-2H-2-chromenone 9(a-j) have been synthesized and tested for their antibacterial activity against human pathogenic strains. The antibacterial evaluation data revealed that the compounds containing 4-methoxyphenyl, 4-fluorophenyl, 4-nitrophenyl and 4-hydroxyphenyl moieties at 4-position of the piperazine ring exhibited potent inhibitory activity towards all the tested bacterial strains. Further, the compounds containing phenyl and 4-methylphenyl moieties showed good activity towards P. aeruginosa and C. violaceum. The 4-nitrophenyl moiety also showed potent activity towards B. subtilis and B. sphaericus.

scholarly journals Design and Synthesis of Bis-pyrimidines Linked with Thiazolidin-4-one as New Antibacterial Agents

2019 ◽  
Vol 31 (9) ◽  
pp. 1913-1918
Author(s):  
Ch. Sanjeeva Reddy ◽  
A. Nagaraj ◽  
V. Yakub ◽  
B. Kalyani
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Antibacterial Agents ◽  
The Other ◽  
Good Activity ◽  
Minimal Inhibitory Concentrations ◽  
Design And Synthesis ◽  
Antibacterial Screening ◽  
Inhibition Zones ◽  
Potent Inhibitory Activity

A series of novel 3-4-[2-hydroxy-5-(4-hydroxy-3-2-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-6-phenyl-4-pyrimidinylbenzyl)phenyl]-6-phenyl-2-pyrimidinyl-2-(aryl)-1,3-thiazolan-4-ones 5(a-j) have been synthesized and assayed for their antibacterial activity against B. subtilis, B. sphaericus, S. aureus, P. aeruginosa, K. Aerogenes and C. violaceum. The inhibition zones and minimal inhibitory concentrations were measured and compared with the streptomycin. The antibacterial screening data reveal that the compounds containing 4-nitrophenyl (5c), 3-nitrophenyl (5d), 4-dimethylaminophenyl (5g) and 1,3-benzodioxole (5j) moiety at 2-position of the thiazolidin-4-one ring exhibited potent inhibitory activity towards all the tested microorganism, which is higher than streptomycin. The other compounds also showed moderate to good activity.

Synthesis and antibacterial evaluation of novel Schiff's base derivatives of nitroimidazole nuclei as potent E. coli FabH inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (97) ◽  
pp. 54217-54225 ◽  
Author(s):  
Xin Zhang ◽  
Chetan B. Sangani ◽  
Li-Xin Jia ◽  
Pi-Xian Gong ◽  
Fang Wang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Schiff’S Base ◽  
E Coli ◽  
Derivatives Of ◽  
Antibacterial Evaluation ◽  
Potent Inhibitory Activity

Series of novel Schiff's base derivatives have been synthesized. Compound 10q showed the most potent inhibitory activity (IC50 = 2.6883 μM).

scholarly journals Identification of Novel Benzoxa-[2,1,3]-diazole Substituted Amino Acid Hydrazides as Potential Anti-Tubercular Agents

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 811
Author(s):  
Alistair Brown ◽  
Ahmed Aljohani ◽  
Jason Gill ◽  
Patrick Steel ◽  
Jonathan Sellars
Keyword(s):  
Antibacterial Activity ◽  
Mycobacterium Tuberculosis ◽  
Amino Acid ◽  
Mtt Assay ◽  
Inhibitory Activity ◽  
Mammalian Cells ◽  
Antibacterial Agents ◽  
Clinical Importance ◽  
Global Burden ◽  
Bacterial Strains

Discovery and development of new therapeutic options for the treatment of Mycobacterium tuberculosis (Mtb) infection are desperately needed to tackle the continuing global burden of this disease and the efficacy and cost limitations associated with current medicines. Herein, we report the synthesis of a series of novel benzoxa-[2,1,3]-diazole substituted amino acid hydrazides in a two-step synthesis and evaluate their inhibitory activity against Mtb and selected bacterial strains of clinical importance utilising an end point-determined REMA assay. Alongside this, their potential for undesired cytotoxicity against mammalian cells was assessed employing standard MTT assay methodologies. It has been demonstrated using modification at three sites (the hydrazine, amino acid, and the benzodiazole) it is possible to change both the antibacterial activity and cytotoxicity of these molecules whilst not affecting their microbial selectivity, making them attractive architectures for further exploitation as novel antibacterial agents.

scholarly journals Pharmacognostical and Antibacterial Evaluation of Murraya koenigii (L) Spreng

2014 ◽  
Vol 22 ◽  
pp. 44-50
Author(s):  
G. Savitha ◽  
S. Balamurugan
Keyword(s):  
Antibacterial Activity ◽  
Human Beings ◽  
Phytochemical Screening ◽  
Bacterial Strains ◽  
Murraya Koenigii ◽  
Medicinal Uses ◽  
Traditional Medicines ◽  
The Family ◽  
Antibacterial Evaluation

Our present study was aimed to detect the medicinal uses of the plant Murraya koenigii (L) Spreng belonging to the family Rutaceae by performing various studies such as Pharmacognostical, phytochemical and antibacterial activity, using seven different bacterial strains, which are harmful to human beings. The Murraya koenigii commonly known as “Curry leaf“ has been recognized in different systems of traditional medicines for the treatment of different diseases and ailments of human beings. The leaves of the plant are said to be cooling and stomachache. The study includes macroscopy, microscopy, preliminary phytochemical screening and antibacterial evaluation

scholarly journals An in vitro Antibacterial Study of Savory Essential Oil and Geraniol in Combination with Standard Antimicrobials

2014 ◽  
Vol 9 (11) ◽  
pp. 1934578X1400901 ◽  
Author(s):  
Dragoljub L. Miladinović ◽  
Budimir S. Ilić ◽  
Branislava D. Kocić ◽  
Marija D. Miladinović
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Antibacterial Study ◽  
Synergistic Interactions ◽  
In Vitro Antibacterial Activity ◽  
Checkerboard Assay

The chemical composition and antibacterial activity of Satureja kitaibelii Wierzb. ex Heuff. (savory) essential oil were examined, as well as the association between it and standard antimicrobials: tetracycline and chloramphenicol. The antibacterial activities of geraniol, the main constituent of S. kitaibelii oil, individually and in combination with standard antimicrobials were also determined. The interactions of the essential oil and geraniol with antimicrobials toward five selected strains were evaluated using the microdilution checkerboard assay in combination with chemometric methods. Oxygenated monoterpenes were the most abundant compound class in the oil (59.7%), with geraniol (50.4%) as the major compound. The essential oil exhibited in vitro antibacterial activity against all tested bacterial strains, but the activities were lower than those of the standard antimicrobials. The combinations savory oil-chloramphenicol, savory oil-tetracycline and geraniol-chloramphenicol produced predominantly synergistic interactions (FIC indices in the range 0.21–0.87) and substantial reductions in the MIC values of antimicrobials against Gram-negative bacteria, the pharmacological treatment of which is very difficult nowadays. In the PCA and HCA analyses these combinations form a separate group.

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

2019 ◽  
Vol 16 (9) ◽  
pp. 723-734
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana R. Katiki ◽  
Kommula Dileep ◽  
C. Ganesh Kumar ◽  
G. Narender Reddy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Reference Drug ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

Extraction and characterization of sea anemones compound and its Anti bacterial and hemolytic studies

2020 ◽  
Vol 10 (4) ◽  
pp. 93-97
Author(s):  
Anil Kumar A ◽  
Raja Sheker K ◽  
Naveen B ◽  
Abhilash G ◽  
Akila CR
Keyword(s):  
Antibacterial Activity ◽  
Focal Point ◽  
Haemolytic Activity ◽  
Klebsiella Pneumonia ◽  
Bacterial Strains ◽  
Sea Anemones ◽  
Marine Plants ◽  
Heteractis Magnifica ◽  
Trididemnum Solidum

Seas assets that give us a variety of characteristic items to control bacterial, contagious and viral ailment and mostly utilized for malignancy chemotherapy practically from spineless creatures, for example, bryozoans, wipes, delicate corals, coelenterates, ocean fans, ocean bunnies, molluscs and echinoderms. In the previous 30 - 40 years, marine plants and creatures have been the focal point of overall endeavours to characterize the regular results of the marine condition. Numerous marine characteristic items have been effectively exceptional to the last phases of clinical preliminaries, including dolastatin-10, a group of peptides disengaged from Indian ocean rabbit, Dollabella auricularia. Ecteinascidin-743 from mangrove tunicate Ecteinascidia turbinata, Didemnins was isolated from Caribbean tunicate Trididemnum solidum and Conopeptides from cone snails (Conus sp.), and a developing number of up-and-comers have been chosen as promising leads for expanded pre-clinical appraisals. Sea anemones possess numerous tentacles containing stinging cells or cnidocytes. The stinging cells are equipped with small organelles known as nematocysts. The two species of sea anemones namely, Heteractis magnificaandStichodactyla haddoni, were collected from Mandapam coastal waters of Ramanathapuram district, Tamilnadu, India. The Nematocyst was collected and centrifuged, and the supernatant was lyophilized and stored for further analysis. The amount of protein from Heteractis Magnifica and Stichodactyla haddoni was estimated. The crude extract has shown haemolytic activity on chicken blood and goat blood. In the antibacterial activity of the sea anemone against six bacterial strains Staphylococcus aureus, Salmonella typhii, Salmonella paratyphii, Klebsiella pneumonia, Vibrio cholerae, Pseudomonas aeruginosa. Antibacterial activity of H. Magnifica and S.haddoni was measured as the radius of the zone of inhibition.

Antioxidant and Antibacterial Activities of Artemisia herba-alba Asso Essential Oil from Middle Atlas, Morocco

2018 ◽  
Vol 16 (S1) ◽  
pp. S48-S54
Author(s):  
Y. Ez zoubi ◽  
S. Lairini ◽  
A. Farah ◽  
K. Taghzouti ◽  
A. El Ouali Lalami
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Foodborne Pathogens ◽  
Food Systems ◽  
Antibacterial Activities ◽  
Culture Collection ◽  
Bornyl Acetate ◽  
Bacterial Strains ◽  
Disk Diffusion Assay ◽  
Different Strains

The purpose of this study was to determine the chemical composition and to evaluate the antioxidant and antibacterial effects of the Moroccan Artemisia herba-alba Asso essential oil against foodborne pathogens. The essential oil of Artemisia herba-alba was analyzed by gas chromatography coupled with mass spectroscopy. The antibacterial activity was assessed against three bacterial strains isolated from foodstuff and three bacterial strains referenced by the ATCC (American Type Culture Collection) using the disk diffusion assay and the macrodilution method. The antioxidant activity was evaluated using the DPPH (2, 2-diphenyl-1- picrylhydrazyl) method. The fourteen compounds of the Artemisia herba-alba essential oil were identified; the main components were identified as β-thujone, chrysanthenone, α-terpineol, α-thujone, α-pinene, and bornyl acetate. The results of the antibacterial activity obtained showed a sensitivity of the different strains to Artemisia herba-alba essential oil with an inhibition diameter of 8.50 to 17.00 mm. Concerning the MICs (minimum inhibitory concentrations), the essential oil exhibited much higher antibacterial activity with MIC values of 2.5 μl/ml against Bacillus subtilis ATCC and Lactobacillus sp. The essential oil was found to be active by inhibiting free radicals with an IC50 (concentration of an inhibitor where the response is reduced by half) value of 2.9 μg/ml. These results indicate the possible use of the essential oil on food systems as an effective inhibitor of foodborne pathogens, as a natural antioxidant, and for potential pharmaceutical applications. However, further research is needed in order to determine the toxicity, antibacterial, and antioxidant effects in edible products.

Lipids and Free Fatty Acids of Red Sea Avrainvillea amadelpha, Holothuria atra, and Sarcocornia fruticosa Inhibit Marine Bacterial Biofilms

2020 ◽  
Vol 17 (6) ◽  
pp. 466-471
Author(s):  
Usama W. Hawas ◽  
Fekri Shaher ◽  
Mohamed Ghandourah ◽  
Lamia T. Abou El-Kassem ◽  
Sathianeson Satheesh ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Free Fatty Acids ◽  
Red Sea ◽  
Inhibitory Activity ◽  
Sea Cucumber ◽  
Bacterial Biofilms ◽  
Antibiofilm Activity ◽  
Bacterial Strains ◽  
Holothuria Atra ◽  
Sarcocornia Fruticosa

This study aimed at evaluating the antibiofilm activity of the Red Sea metabolites from green alga Avrainvillea amadelpha, sea cucumber Holothuria atra and costal plant Sarcocornia fruticosa against three biofilm bacterial strains isolated from Jeddah coast. Free fatty acids (FFAs) and other lipoidal matters were extracted from these organisms and analyzed by GC-MS. The composition of lipoidal fractions showed that A. amadelpha is rich by 74% saturated FAs, while sea cucumber H. atra revealed high content (60%) of unsaturated FAs. Palmitic acid is the major FA component in all species ranging from 14.5 to 26.7%. Phytol, sterols and hydrocarbons (C8-C29) were represented in the alga A. amadelpha as high contents with values 25.8, 21.9 and 18.5%, respectively. The extracts and lipoidal contents showed biofilm inhibitory activity against the isolated bacterial strains, where the unsaponified lipoidal fraction of S. fruticosa exhibited highest inhibitory activity against Planomicrobium sp. at concentration of 200 µg/mL.

Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity

2020 ◽  
Vol 17 (5) ◽  
pp. 396-403
Author(s):  
Nalla Krishna Rao ◽  
Tentu Nageswara Rao ◽  
Botsa Parvatamma ◽  
Y. Prashanthi ◽  
Ravi Kumar Cheedarala
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Sodium Acetate ◽  
Good Activity ◽  
Activity Profile ◽  
Aryl Aldehydes ◽  
Chemical Structures ◽  
Novel Synthesis ◽  
Target Molecules

Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. Objective: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. Methods: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. Results: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. Conclusion: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.

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