scholarly journals Design, Synthesis, and Antimicrobial Activities of 1,2,3-Triazole Glycoside Clickamers

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 790 ◽  
Author(s):  
Tamer El Malah ◽  
Hany F. Nour ◽  
Amira A. E. Satti ◽  
Bahaa A. Hemdan ◽  
Wael A. El-Sayed
Keyword(s):  
Staphylococcus Aureus ◽  
Antifungal Activity ◽  
Bacterial Resistance ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Spectroscopic Techniques ◽  
Reference Drug ◽  
Chemical Structures

Bacterial resistance remains a significant threat and a leading cause of death worldwide, despite massive attempts to control infections. In an effort to develop biologically active antibacterial and antifungal agents, six novel aryl-substituted-1,2,3-triazoles linked to carbohydrate units were synthesized through the Cu(I)-catalyzed azide-alkyne cycloaddition CuAAC of substituted-arylazides with a selection of alkyne-functionalized sugars. The chemical structures of the new derivatives were verified using different spectroscopic techniques. The novel clicked 1,2,3-triazoles were evaluated for in vitro antibacterial activity against Gram-positive Staphylococcus aureus and Gram-negative Pseudomonas aeruginosa, and the obtained results were compared with the activity of the reference antibiotic “Ampicillin”. Likewise, in vitro antifungal activity of the new 1,2,3-triazoles was investigated against Candida albicans and Aspergillus niger using “Nystatin” as a reference drug. The results of the biological evaluation pointed out that Staphylococcus aureus was more susceptible to all of the tested compounds than other examined microbes. In addition, some tested compounds exhibited promising antifungal activity.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

Synthesis and Antimicrobial Evaluation of Amino Acid Naphthoquinone Derivatives as Potential Antibacterial Agents

Chemotherapy ◽  
2021 ◽  
Author(s):  
Lluvia Itzel López-López ◽  
Ernesto Rivera-Ávalos ◽  
Cecilia Villarreal-Reyes ◽  
Fidel Martínez-Gutiérrez ◽  
Denisse de Loera
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Culture Collection ◽  
Anticancer Activities ◽  
Broth Microdilution Method

Background: The synthesis and biological evaluation of 1,4-naphthoquinone derivatives are of great interest since these compounds exhibit strong antibacterial, antifungal, antimalarial, and anticancer activities. The electronic properties of naphthoquinones are usually modulated by attaching functional groups containing nitrogen, oxygen and sulfur atoms, which tune their biological potency and selectivity. Methods: A series of 13 amino acid 1,4-naphthoquinone derivatives were synthesized under assisted microwave and ultrasound conditions. The antibacterial activity compounds was tested against American type Culture Collection (ATCC): Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis, as well two multidrug resistant pathogens: Escherichia coli and Staphylococcus aureus from clinical isolated. Minimal inhibitory concentration (MIC) was determined using the broth microdilution method. Results: MIC of derivatives 4–11, 14 and 16 showed antimicrobial activity against gram-positive and gram-negative bacteria. Antimicrobial activities of the compounds 4–8 and 14 were ≤MIC 24.7 μg∙mL-1 against all the reference strain, even more the compound 6 showed the most potent activity with a MIC of 3.9 μg∙mL-1 on S. aureus. On the clinical isolated the compounds 7, 8 and 14 showed a MIC of 49.7 and 24.7 μg∙mL-1 against S. aureus y E. coli respectively. About ADME properties and Osiris analysis, the compounds 4-16 presented high gastrointestinal absorption and good characteristics for oral bioavailability and the compound 14 was the less toxic. Conclusion: amino acid 1,4-naphthoquinone derivatives showed good in vitro antibacterial activity against clinical strains, and modifications on C-3 with cloride atom enhanced the efficiency against same pathogens.

Synthesis and Biological Evaluation of Novel 5-Oxo-1-Phenylpyrrolidine-3-Carboxylic Acid Analogs

Drug Research ◽  
2018 ◽  
Vol 69 (05) ◽  
pp. 271-276
Author(s):  
Poornima Devi ◽  
Abha Bishnoi ◽  
Krishna Srivastava ◽  
Sunil Kumar ◽  
Ankita Srivastava ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Carboxylic Acid ◽  
Biological Evaluation ◽  
Good Activity ◽  
Pyrrolidine Ring ◽  
Gram Negative ◽  
Chemical Structures ◽  
Antibacterial Screening ◽  
Synthesis And Biological Evaluation

AbstractA number of 5-oxo-1-phenyl-4-(substituted methyl) pyrrolidine-3-carboxylic acid derivatives bearing pyrrolidine ring and methylamino residues in their structure were synthesized as potential antibacterial drugs. The chemical structures of all the compounds were established by their UV-Vis absorption spectroscopy, IR, 1H, 13C NMR and mass spectroscopy. The in vitro antibacterial screening of all novel compounds was done against gram-positive Staphylococcus aureus, Bacillus subtilis and gram-negative Pseudomonas aeruginosa. The results revealed that compounds 5d, e, f and g showed moderate to good activity against the tested microbes.

scholarly journals Design, synthesis and biological evaluation of new substituted benzofuran-based derivatives via C−H bond activation

2020 ◽  
Vol 85 (11) ◽  
pp. 1405-1415
Author(s):  
Behjat Pouramiri ◽  
Mahboobeh Zahedifar ◽  
Adileh Ayati ◽  
Farah Pouramiri ◽  
Mahdiyeh Ahmadi
Keyword(s):  
Bond Activation ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Spectroscopic Methods ◽  
Design Synthesis ◽  
Activation Reaction ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation

A series of biologically active disubstituted benzofuran derivatives (3a?d) have been designed and synthesized via C?H bond activation reaction. The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro anti acetylcholinesterase (AChE) activities of these novel compounds were evaluated and showed low to moderate results. Among them, compound 3d moderately inhibited AChE activities with 68.12 % value.

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.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

Efficient Synthesis of Novel N-[4-Methyl-3-(4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl)thiazol-2(3H)-ylidene]benzamide Hybrid Ring System as Potential Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Hummera Rafique ◽  
Aamer Saeed ◽  
Muhammad Naseem ◽  
Tauqeer Riaz ◽  
Fouzia Perveen ◽  
...  
Keyword(s):  
Bacterial Resistance ◽  
Antioxidant Activities ◽  
Antibacterial Properties ◽  
Antibacterial Activities ◽  
Structural Features ◽  
Ring System ◽  
Biologically Active ◽  
Thiazole Ring ◽  
Spectroscopic Techniques ◽  
Hybrid Ring

Background: Heterocyclic compounds display versatile biological applications, so the aim of this paper was to prepare biologically important heterocycles with enhanced bacterial resistance and to evaluate for their various structural features that are responsible for their biological properties. Objective: The objective was to synthesize bacterial resistance compounds with enhanced antibacterial properties. Method: Ester moiety containing thiazole ring was converted into its hydrazide derivatives. These heterocyclic derivatives were cyclized into another ring oxadiazole; hence a hybrid ring system of two biologically active rings was prepared. Result: All the synthesized compounds were characterized by spectroscopic techniques and were screened for their antibacterial potential; they possess significant antibacterial activities. Conclusion: New hybrid heterocyclic ring systems were synthesized by cyclization of hydrazide derivatives by adopting two step strategy in good yields. All the synthesized compounds were evaluated for their antioxidant activities; they showed moderate to significant activities. QSAR and Molecular docking studies were performed to determine the mode of interaction. Experimental and computational data is in accordance with the determined antibacterial activities.

scholarly journals Synthesis and Biological Evaluation of Aminonaphthols Incorporated Indole Derivatives

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Saundane Anand Raghunath ◽  
Kirankumar Nandibeoor Mathada
Keyword(s):  
Radical Scavenging ◽  
Antitubercular Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Secondary Amines ◽  
Anticancer Activities ◽  
One Pot ◽  
Antioxidant Power ◽  
Mic Value

An efficient one pot condensation of naphthols (1), 2,5-disubstituted indole-3-carboxaldehydes (2), and secondary amines (3) has been achieved using dichloromethane as a solvent, stirring at room temperature. Some of the new [(disubstituted amino)(5-substituted 2-phenyl-1H-indol-3-yl)methyl]naphthalene-ols (4) derivatives were prepared in good yields. The significant features of this method are simple work-up procedure, inexpensive nontoxic solvent, shorter reaction times, and excellent product yields. The structures of newly synthesized compounds (4a–r) are confirmed by their elemental analysis, FTIR, 1H and 13C NMR, and mass spectral data. These compounds were screened for their in vitro antioxidant, antimicrobial, antitubercular, and anticancer activities. Among the synthesized compounds (4a–r), the compound 4e exhibited highest activity for radical scavenging and ferric ions reducing antioxidant power activities; compounds 4b, 4h, and 4k showed good metal chelating activity. Compounds 4n and 4q showed excellent antimicrobial activities with MIC value 08 µg/mL against tested strains. Compounds 4h, 4k, 4n, and 4q exhibited promising antitubercular activity with MIC value 12.5 µg/mL. Compounds 4k and 4q exhibited 100% cell lysis at concentration 10 µg/mL against MDA-MB-231 (human adenocarcinoma mammary gland) cell lines.

scholarly journals Antibacterial Effect of Silver Nanoparticles on Klebsiella spp

2020 ◽  
Vol 1 (2) ◽  
pp. 8-15
Author(s):  
Gislanne Stéphanne Estevam da Silva ◽  
Rivaldo Leon Bezerra Cabral ◽  
Nathalie de Sena Pereira ◽  
José Heriberto Oliveira do Nascimento ◽  
Dany G kramer
Keyword(s):  
Silver Nanoparticles ◽  
Bacterial Resistance ◽  
Brain Heart Infusion ◽  
Trisodium Citrate ◽  
Antimicrobial Activities ◽  
Positive Control ◽  
Negative Control ◽  
In Vitro Tests ◽  
Klebsiella Spp

Silver nanoparticles (AgNP) can be incorporated into medical devices, such as tissues, to circumvent bacterial resistance such as Klebsiella spp, which can lead to skin and mucosal infections. Thus, the aim of the present study was to synthesize silver nanoparticles for later incorporation into cotton fabrics and in vitro tests against Klebsiella spp. The AgNP colloidal solution was synthesized (AgNO3 - 0.1 mM, 100 mM trisodium citrate, polyvinylpyrrolidone - 0.24 g, H2OH2) and then impregnated into the cotton fabric pretreated with poly diallyl dimethylammonium chloride (PDDA) of 100/500 tissue, shaken for 30 minutes). The material produced was analyzed by the FTIR; DLS and reflectance spectroscopy. The tests of the antimicrobial activities were by the microdilution technique against Klebsiella spp, in tubes containing Brain Heart Infusion (BHI), with the solution of silver (1); Tissue containing AgNP - 4 mm (2); Negative control (3) and positive control - ceftriaxone (4). Regarding MIC, the inhibitory activity occurred of the dilutions between 1/2 and 1/16. The AgNP particles had an average size of 24.75 nm. As synthesized AgNPs demonstrate the excellent antimicrobial activity against Klebsiella spp, with special emphasis on applications in nanotechnology and nanomedicine, targeting multiresistant antibiotic bacteria.

scholarly journals Phytochemical Characterization and Evaluation of Biological Activities of Egyptian Carob Pods (Ceratonia siliqua L.) Aqueous Extract: In Vitro Study

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Phytochemical Analysis ◽  
Type I ◽  
Hypotonic Solution ◽  
Ceratonia Siliqua

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.

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