Synthesis and Structural Elucidation of Aminoacetylenic Derivatives of 7-Methoxy- 2-Naphthole as Antimicrobial Agents

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Abu- Safieh Rana ◽  
Muhi- Eldeen Zuhair ◽  
Alsarahni Aseel ◽  
Al-Kaissi Elham
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Naphthalene Derivatives ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi ◽  
Aminoacetylenic Derivatives ◽  
Derivatives Of ◽  
Mic Value

A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 µg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 µg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125µg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 µg/ml, all compounds have the same MIC value against P. aeruginosa (125 µg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 µg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi.

scholarly journals Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity

2008 ◽  
Vol 58 (1) ◽  
pp. 29-42 ◽  
Author(s):  
Rafat Mohareb ◽  
Hanaa Hana
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Dimethyl Acetal ◽  
Dimethyl Formamide ◽  
Gram Positive Bacteria ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Potential Antimicrobial Activity

Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. Thein vitroantimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.

scholarly journals Novel Zinc(II) Complexes of Heterocyclic Ligands as Antimicrobial Agents: Synthesis, Characterisation, and Antimicrobial Studies

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Ramesh S. Yamgar ◽  
Y. Nivid ◽  
Satish Nalawade ◽  
Mustapha Mandewale ◽  
R. G. Atram ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Metal Complexes ◽  
Antimicrobial Agents ◽  
Spectroscopic Techniques ◽  
Schiff Base Ligands ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Antimicrobial Studies

The synthesis and antimicrobial activity of novel Zn(II) metal complexes derived from three novel heterocyclic Schiff base ligands 8-[(Z)-{[3-(N-methylamino)propyl]imino}methyl]-7-hydroxy-4-methyl-2H-chromen-2-one, 2-[(E)-{[4-(1H-1,2,4-triazol-1-ylmethyl)phenyl]imino}methyl]phenol, and (4S)-4-{4-[(E)-(2-hydroxybenzylidene)amino]benzyl}-1,3-oxazolidin-2-one have been described. These Schiff base ligands and metal complexes are characterised by spectroscopic techniques. According to these data, we propose an octahedral geometry to all the metal complexes. Antimicrobial activity of the Schiff base ligand and its metal complexes was studied against Gram negative bacteria:E. coliandPseudomonas fluorescens, Gram positive bacteria:Staphylococcus aureus,and also against fungi, that is,C. albicansandA. niger. Some of the metal complexes show significant antifungal activity (MIC < 0.2 μg/mL). The “in vitro” data has identified [Zn(NMAPIMHMC)2]·2H2O, [Zn(TMPIMP)2]·2H2O, and [Zn(HBABO)2]·2H2O as potential therapeutic antifungal agents againstC. albicansandA. niger.

scholarly journals Novel (+)-Neoisopulegol-Based O-Benzyl Derivatives as Antimicrobial Agents

2021 ◽  
Vol 22 (11) ◽  
pp. 5626
Author(s):  
Tam Minh Le ◽  
Thu Huynh ◽  
Fatima Zahra Bamou ◽  
András Szekeres ◽  
Ferenc Fülöp ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Substituent Effects ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Gram Positive Bacteria ◽  
Urgent Task ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Discovery of novel antibacterial agents with new structures, which combat pathogens is an urgent task. In this study, a new library of (+)-neoisopulegol-based O-benzyl derivatives of aminodiols and aminotriols was designed and synthesized, and their antimicrobial activity against different bacterial and fungal strains were evaluated. The results showed that this new series of synthetic O-benzyl compounds exhibit potent antimicrobial activity. Di-O-benzyl derivatives showed high activity against Gram-positive bacteria and fungi, but moderate activity against Gram-negative bacteria. Therefore, these compounds may serve a good basis for antibacterial and antifungal drug discovery. Structure–activity relationships were also studied from the aspects of stereochemistry of the O-benzyl group on cyclohexane ring and the substituent effects on the ring system.

Synthesis and Antimicrobial Evaluation of 2-(Substituted-phenyl)-3-(4-(4- Nitrophenyl)Thiazol-2-yl)Thiazolidin-4-One Derivatives

2019 ◽  
Vol 15 (1) ◽  
pp. 114-119 ◽  
Author(s):  
Rakesh Kumar ◽  
Shailendra Patil
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Public Health Issue ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Microbial Infections ◽  
Antimicrobial Evaluation ◽  
Potential Antimicrobial Activity ◽  
Tube Dilution

Background:Diseases caused by microbial infections are very common worldwide. Although the search of innovative antimicrobial agents is the current focus for the researchers, the treatment of infectious diseases remains an important public health issue and a challenging problem in front of medicinal chemist.Methods:A series of 2-(4-hydroxyphenyl)-3-(4-(4-nitrophenyl) thiazol-2-yl)thiazolidin-4-one derivatives (T1-T10) was designed and synthesized. All the titled compounds were evaluated for their antimicrobial potential. Antimicrobial activity was performed by tube dilution methods against Gram negative Escherichia coli MTCC 443 (E. Coli), Gram positive bacteria: Staphylococcus aureus MTCC 3160 (S. aureus) and Bacillus subtilis MTCC 441 (B. Subtilis), and fungal strains: Aspergillus niger MTCC 281 (A. niger) and Candida albicans MTCC 227 (C. albicans).Results:Among the synthesized derivatives, compounds 2, 4 and 10 were found to be most active antimicrobial agents.Conclusion:In conclusion, a series of 2-(phenyl)-3-(4-(phenyl)thiazol-2-yl)thiazolidin-4-ones have been designed and synthesized. All the titled compounds were evaluated for their in vitro antimicrobial activity against five representative microorganisms. The results of antimicrobial study indicated that the presence of nitro and chloro groups in aromatic ring improved antibacterial activity, whereas the presence of hydroxy group improved antifungal activity of substituted 4-thiazolidinone derivatives.

scholarly journals Synthesis and Evaluation of Some Coumarin Based Schiff's Bases as Potential Antimicrobial Agents'

2012 ◽  
Vol 9 (4) ◽  
pp. 2079-2088 ◽  
Author(s):  
Vishakha Bansode ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the title compounds 3-(4-(4, 5-dihydro-5-(substituted phenyl)-1H-3-pyrazolyl) phenylimino) methyl)-4-chloro-2H-chromen-2-one 5(a-g) have been synthesized. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive bacteria, gram negative bacteria and fungi. The compound (5b) was found to be the most active with MIC of 20 µg/ml against all the tested organisms.

scholarly journals Synthesis, Antimicrobial Activity and Molecular Docking of Novel Thiourea Derivatives Tagged with Thiadiazole, Imidazole and Triazine Moieties as Potential DNA Gyrase and Topoisomerase IV Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2766 ◽  
Author(s):  
Heba E. Hashem ◽  
Abd El-Galil E. Amr ◽  
Eman S. Nossier ◽  
Elsayed A. Elsayed ◽  
Eman M. Azmy
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Topoisomerase Iv ◽  
Thiourea Derivatives ◽  
E Coli ◽  
Cytotoxicity Studies ◽  
Ic50 Values

To develop new antimicrobial agents, a series of novel thiourea derivatives incorporated with different moieties 2–13 was designed and synthesized and their biological activities were evaluated. Compounds 7a, 7b and 8 exhibited excellent antimicrobial activity against all Gram-positive and Gram-negative bacteria, and the fungal Aspergillus flavus with minimum inhibitory concentration (MIC) values ranged from 0.95 ± 0.22 to 3.25 ± 1.00 μg/mL. Furthermore, cytotoxicity studies against MCF-7 cells revealed that compounds 7a and 7b were the most potent with IC50 values of 10.17 ± 0.65 and 11.59 ± 0.59 μM, respectively. On the other hand, the tested compounds were less toxic against normal kidney epithelial cell lines (Vero cells). The in vitro enzyme inhibition assay of 8 displayed excellent inhibitory activity against Escherichia coli DNA B gyrase and moderate one against E. coli Topoisomerase IV (IC50 = 0.33 ± 1.25 and 19.72 ± 1.00 µM, respectively) in comparison with novobiocin (IC50 values 0.28 ± 1.45 and 10.65 ± 1.02 µM, respectively). Finally, the molecular docking was done to position compound 8 into the E. coli DNA B and Topoisomerase IV active pockets to explore the probable binding conformation. In summary, compound 8 may serve as a potential dual E. coli DNA B and Topoisomerase IV inhibitor.

Screening of Antimicrobial Activity and Cytotoxic Effects of Two Cladonia Species

2013 ◽  
Vol 68 (5-6) ◽  
pp. 191-197 ◽  
Author(s):  
Birkan Açıkgöz ◽  
İskender Karaltı ◽  
Melike Ersöz ◽  
Zeynep M. Coşkun ◽  
Gülşah Çobanoğlu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Chloroform Extract ◽  
Cytotoxic Effects ◽  
Minimal Inhibitory Concentrations ◽  
E Coli ◽  
Methanol Extracts ◽  
Gram Positive Bacteria

The present study explores the antimicrobial activity and cytotoxic effects in culture assays of two fruticose soil lichens, Cladonia rangiformis Hoffm. and Cladonia convoluta (Lamkey) Cout., to contribute to possible pharmacological uses of lichens. In vitro antimicrobial activities of methanol and chloroform extracts against two Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), two Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus), and the yeast Candida albicans were examined using the paper disc method and through determination of minimal inhibitory concentrations (MICs). The data showed the presence of antibiotic substances in the chloroform and the methanol extracts of the lichen species. The chloroform extracts exhibited more signifi cant antimicrobial activity than the methanol extracts. However, a higher antifungal activity was noted in the methanol extract of C. rangiformis. The maximum antimicrobial activity was recorded for the chloroform extract of C. convoluta against E. coli. The cytotoxic effects of the lichen extracts on human breast cancer MCF-7 cells were evaluated by the trypan blue assay yielding IC50 values of ca. 173 and 167 μg/ml for the extracts from C. rangiformis and C. convoluta, respectively.

scholarly journals Phytochemical characterization, anti-cancer and antimicrobial activity of isolated fractions of Alysicarpus vaginalis

2017 ◽  
Vol 12 (1) ◽  
pp. 77 ◽  
Author(s):  
Ganesh Tapadiya ◽  
Mayura A. Kale ◽  
Shweta Saboo
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Methanolic Extract ◽  
Hep G2 ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Anti Cancer ◽  
Proliferative Assay ◽  
Bacteria And Fungi

<p class="Abstract">The methanolic extract of <em>Alysicarpus </em>vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for<em> in vitro</em> antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC<sub>50 </sub>values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and<em> E. coli</em> whereas chloroform and n-butanol fractions were more effective against <em>S. aureus</em> and <em>B. </em>subtilis. The phytochemical characterization by HPLC analysis indicated the presence of important polyphenolic and steroidal compounds.</p>

scholarly journals Synthesis and Antimicrobial Evaluations of Sulfur Inserted Fluoro-Benzimidazoles

2021 ◽  
Vol 33 (7) ◽  
pp. 1525-1529
Author(s):  
Parmesh Kumar Dwivedi ◽  
Devdutt Chaturvedi
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Strains ◽  
Substituted Anilines ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
New Compounds ◽  
Derivatives Of ◽  
Multiple Step

A new series of fluorinated sulfur inserted benzimidazole analogues Za-i were synthesized and characterized. The new compounds were screened for their antimicrobial and antioxidant potential. The synthesized compounds were obtained by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol X. The compounds Ya-i prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF. Finally, the compound X was reacted with different derivatives of 2-chloro-N-phenylacetamide resulting in formation of titled compounds Za-i. The synthesized compounds (Za-Zi) were characterized by spectral analysis viz.1H & 13C NMR, mass spectra, elemental analysis and IR. The in vitro antimicrobial potential against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans) was recorded for the obtained compounds. Some of the compounds exhibited encouraging results (in MIC) against Gram-positive and Gram-negative bacterial strains. These studies thus suggest that the designed sulfur inserted fluoro-benzimidazoles scaffold may serve as new promising template for further amplification as antimicrobial agents.

Preparation of a Novel Complex Antimicrobial Agent and its Antimicrobial Activity In Vitro

2012 ◽  
Vol 550-553 ◽  
pp. 1030-1038
Author(s):  
Peng Li ◽  
Wei Guo Wang ◽  
Yu Jia Cui ◽  
Yong Liang Zhao ◽  
Ya Nan Gu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antimicrobial Agent ◽  
Antimicrobial Agents ◽  
E Coli ◽  
Orthogonal Experiments ◽  
Novel Complex ◽  
Cefoperazone Sodium ◽  
Complex Antimicrobial Agent

Purpose To develop a novel complex antimicrobial agent and determine the optimal components of the composite antimicrobial agents and its antimicrobial activity in vitro. Methods According to antimicrobial mechanisms，antibacterial spectrums，physical and chemical properties and applicabilities of existing antimicrobial agents in clinical use, select out cefoperazone sodium, sulbactam sodium and cephradine as the basic components to make a novel complex antimicrobial agent. Utilize yeast, staphylococcus aureus and E. coli bacteria as test bacteria. Do the three factors four-level orthogonal experiments by the maximum amount, the middle amount, low amount and Minimum amount of the three-component agent to research the optimum ratio of the drug. Measure the titer of the compound antimicrobial agent by the way of tube-plate method (2 doses). With known contents of Penicillin Sodium for Injection as control, and determine its minimum inhibitory concentration against staphylococcus aureus, E. coli and yeast by using the agar doubling dilution method. The experimental results were analysized by statistical analysis software SPSS16.0. Results The results of the three factors four-level orthogonal experiments indicate the optimum ratios of Cefoperazone Sodium, Sulbactam Sodium and Cephradine against E. coli, yeast and staphylococcus aureus were 2:2:3, 1:2:2 and 2:6:5, their titers were 1353.9U/mg, 982.7U/mg and 1015.5U/mg. With the highest titer proportion 2:2:3 as the composition of the antimicrobial compound. This compound antimicrobial agent had a good antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria and Fungi, its minimal inhibitory concentration (MIC) against staphylococcus aureus, E. coli and yeast were 2.000μg/ml, 0.500μg/ml and 16.000μg/ml. Conclusion This research acquires a composite of antibiotics. This antimicrobial compound has a broader spectrum and higher antimicrobial activity in vitro comparing with traditional common single antibiotics, and it especially has a good antimicrobial activity against fungi. The results set a scientific foundation for enriching clinical medicines.

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