scholarly journals Facile Synthesis, Characterization and Antimicrobial Activities of Novel 6-AminoTriazolo-Thiadiazoles Integrated with Benzofuran and Pyrazole Moieties

2019 ◽  
Vol 35 (6) ◽  
pp. 1712-1717
Author(s):  
Mohammad Idrees ◽  
Satish S. Kola ◽  
Naqui J. Siddiqui
Keyword(s):  
Mass Spectra ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Facile Synthesis ◽  
One Pot ◽  
Standard Drug ◽  
Cyclocondensation Reaction ◽  
Aryl Isothiocyanate ◽  
Work Up

In the undertaken research we have reported simple efficient technique to afford a novel series of 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-N-aryl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-amine (4a-g) derivatives obtained by one pot cyclocondensation reaction of 5-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-4-amino-4H-1,2,4-triazole-3-thiol (3) with substituted aryl isothiocyanate in DMF and K2CO3, without formation undesirable side products by simple work up procedure. The structures yielded (4a-g) were established by 13CNMR, IR, 1HNMR, elemental analysis and mass spectra. Entire synthesised compounds were screened for their in-vitro biological assay via microorganism Gram positive and Gram negative bacterial strains at different concentrations. The bioassay revealed that some of the compounds have promising antimicrobial activities when compared with standard drug Chloramphenicol.

scholarly journals Synthesis, Characterization and in vitro Antimicrobial Screening of Some Novel Series of 2-Azetidinone Derivatives Integrated with Quinoline, Pyrazole and Benzofuran Moieties

2020 ◽  
Vol 32 (4) ◽  
pp. 896-900
Author(s):  
M. Idrees ◽  
Y.G. Bodkhe ◽  
N.J. Siddiqui ◽  
S.S. Kola
Keyword(s):  
Mass Spectra ◽  
Pathogenic Bacteria ◽  
Catalytic Amount ◽  
Spectral Studies ◽  
One Pot ◽  
E Coli ◽  
One Pot Condensation ◽  
Cyclocondensation Reaction ◽  
In Vitro Antibacterial Activity

A series of 5-(benzofuran-2-yl)-N-(3-chloro-4-(2-(p-tolyloxy) substituted quinolin-3-yl)-2-oxoazetidin-1-yl)-1-phenyl-1H-pyrazole-3-carboxamide derivatives (4a-f) were synthesized with excellent yields by cyclocondensation reaction of 5-(benzofuran-2-yl)-N′-(2-(p-tolyloxy) substituted quinolin-3-yl)methylene)-1-phenyl-1H-pyrazole-3-carbohydrazide (3a-f) with chloroacetyl chloride in presence of triethylamine in DMF. One pot condensation of 5-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide (1) with 2-(p-tolyloxy) substituted quinoline-3-carbaldehyde (2a-f) in ethanol solvent in presence of catalytic amount of acetic acid gave intermediate compounds (3a-f). The structures of newly synthesized compounds have been substantiated through elemental analysis and spectral studies viz. 1H NMR, 13C NMR, IR and mass spectra. All the synthesized compounds were screened for their in vitro antibacterial activity against pathogenic bacteria such as S. aureus and E. coli at different concentrations.

scholarly journals Thiazolo-Pyrimidine Analogues: Synthesis, Characterization and Docking Studies Guided Antimicrobial Activities

2020 ◽  
Vol 11 (2) ◽  
pp. 9443-9455
Keyword(s):  
Aromatic Aldehydes ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
One Pot ◽  
Standard Drug ◽  
Toluene Sulfonic Acid ◽  
Pyrimidine Analogues

In the current study, bicyclic 1-(7-methyl-3,5-diphenyl-5H-thiazolo(3,2-α)pyrimidine-6-yl)ethanone (4a-l) derivatives have been designed and conveniently synthesized by one-pot three-component method via cyclocondensation of substituted 4-phenylthiazole-2-amine (1a-c), acetylacetone (2) and various aromatic aldehydes (3a-d) in the presence of p-toluene sulfonic acid (PTSA) under acetonitrile solvent medium. The synthesized compounds (4a-l) have been characterized by spectral analysis and subjected to docking study against protein DNA gyrase (PDB Code: 1KZN), and also, the compounds were screened for their in vitro antimicrobial activities. The bioassay of the synthesized compounds envisioned that the compound 4k emerged as a broad-spectrum antibacterial agent, and 4l emerged as a good antifungal agent compared to standard drug.

Microwave Induced one Pot Ugi Multicomponent Reaction of Fluoroquino lone Scaffolds: Their Biological Evaluation

2020 ◽  
Vol 07 ◽  
Author(s):  
Navin B. Patel ◽  
Rahul B. Parmar ◽  
Hetal I. Soni
Keyword(s):  
Multicomponent Reaction ◽  
Mass Spectra ◽  
Antitubercular Activity ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Aspergillus Clavatus ◽  
One Pot ◽  
Concentration Method ◽  
Work Up

Microwave irradiated facile and efficient process for one pot Ugi multicomponent reaction of a novel series of fluoroquinolone scaffolds is described here. On the basis of this approach, a new route to synthesize this privileged scaffolds were designed with higher yields, a clean procedure, time efficient and simple work-up. Our aim is to develop a biologically active fluoroquinolone scaffolds by microwave induced one pot Ugi multicomponent reaction. All the synthesized molecules were characterized by IR, 1H NMR, 13C NMR, and Mass spectra. The antimicrobial activity of synthesized compounds was screened against two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), two Grampositive bacteria (Staphylococcus aureus, Streptococcus pyogenes), and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) utilizing the MIC (Minimal Inhibitory Concentration) method and antitubercular activity H37Rv utilizing L. J. Slope method. Some of these novel derivatives demonstrate moderate to good in vitro antibacterial, antifungal and antitubercular activities.

Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
High Yield ◽  
Breast Cancer Cell Lines ◽  
Pyridine Derivatives ◽  
One Pot ◽  
Standard Drug ◽  
Three Component Reaction ◽  
Anti Cancer

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

scholarly journals Antimicrobial Activity and Chemical Characterization of a Non-Polar Extract of Saffron Stamens in Food Matrix

Foods ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 703
Author(s):  
Severino Zara ◽  
Giacomo L. Petretto ◽  
Alberto Mannu ◽  
Giacomo Zara ◽  
Marilena Budroni ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Fatty Acid Content ◽  
Chemical Characterization ◽  
Antimicrobial Activities ◽  
Added Value ◽  
Gas Chromatography Mass Spectrometry ◽  
Food Matrix ◽  
Bacterial Strains ◽  
By Products

The production of saffron spice generates large quantities of plant by-products: over 90% of the plant material collected is discarded, and a consideration fraction of this waste is plant stamens. This work investigated the chemical composition and the antimicrobial activities of the non-polar fraction extracted from four different saffron flower stamens. The chemical composition of ethereal extracts of the saffron stamens was qualitatively assessed by means of gas–chromatography-mass spectrometry (GC-MS) and nuclear magnetic resonance (NMR) analyses. These analyses revealed ethereal extracts to possess a high polyunsaturated fatty acid content. In vitro antibacterial activity of stamen extracts showed no large differences between Gram-positive and Gram-negative bacteria in terms of minimal inhibitory concentration (MIC). In food matrix microbial analysis of the bacterial strains belonging to the main foodborne pathogen species, including Staphylococcus aureus DSM 20231, Escherichia coli DSM 30083, and Listeria monocytogenes DSM 20600, using low-fat UHT milk, revealed a statistically significant reduction in the number of cells (particularly for E. coli and S. aureus with a complete elimination of the population of the two target bacteria following incubation in diethyl ether extracts of saffron stamen (DES) at high concentrations tested, both at 37 °C and 6 °C (for 48 h and 7 days, respectively). A synergic effect was observed when the pathogens were incubated at 6 °C with DES. This work shows these by-products to be excellent sources of bioactive compounds, which could be exploited in high-added-value products, such as food, cosmetics, and drugs.

scholarly journals In Vitro Assessment of Antioxidant, Thrombolytic, Antimicrobial Activities of Medicinal Plant Pandanus odoratissimus L. Leaves Extract

2020 ◽  
Vol 12 (3) ◽  
pp. 379-390
Author(s):  
F. I. Penu ◽  
S. M. Ivy ◽  
F. Ahmed ◽  
J. Uddin ◽  
M. S. Hossain ◽  
...  
Keyword(s):  
Soluble Fraction ◽  
Blood Clot ◽  
Folk Medicine ◽  
Maximum Level ◽  
Antimicrobial Activities ◽  
Total Phenolic ◽  
Thrombolytic Activity ◽  
Standard Drug ◽  
Pandanus Odoratissimus

The present study was carried out to investigate phytochemical, antioxidant; antimicrobial, thrombolytic activity and estimate total phenolic, total flavonoid content of Pandanus odoratissimus (p.odoratissimus) leaves of methanol extract. In thrombolytic activity, aqueous soluble fraction (AQSF) exhibited highest percentage (46.58 %) of potential to lyse blood clot compared to standard drug streptokinase (69.52 %). In antimicrobial assay, dichloromethane soluble fraction (DCMSF) explored the highest diameter of clear zone of inhibition against both gram positive (19.60 ± 0.12 mm) and gram negative (20.00 ± 0.20 mm) bacteria compared to standard antibiotic, Kanamycin (50.00 ± 0.19). Levels of antioxidant were determined by DPPH assay followed by calculated IC50 values of different Kupchan extracts. The methyl soluble fraction (MSF) showed the lowest level of IC50 value (36.70 ± 0.32 µg/mL) in comparison to ascorbic acid (12.48 ± 0.09 µg/mL) while MSF disclosed the maximum level (62.19 ±  0.26 mg of GAE/g of extract) of total phenolic content in the extracts of P. odoratissimus. This study was conducted to validate the P. odoratissimus leaves used as a folk medicine such as, antioxidant, thrombolytic, and antimicrobial potential.

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 The PHYTOCHEMICALS, ANTIOXIDANT AND ANTIMICROBIAL PROPERTIES OF Senna alata AND Senna tora LEAF EXTRACTS AGAINST BACTERIAL STRAINS CAUSING SKIN INFECTIONS

2019 ◽  
Vol 2 (1) ◽  
pp. 19
Author(s):  
Murni Halim
Keyword(s):  
Leaf Extract ◽  
Antimicrobial Properties ◽  
Inhibition Zone ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Leaf Extracts ◽  
Natural Drugs ◽  
Senna Alata

A study was carried out to screen for phytochemical constituents and assess the antioxidant and antimicrobial activities of Senna alata and Senna tora leaf extracts. The leaves were first dried at room temperature and 50°C in an oven prior to solvent extraction using ethanol and methanol. The in-vitro qualitative assays showed that both S. alata and S. tora leaf extracts contained bioactive and secondary metabolites components such as tannins, steroids, saponin, terpenoids, glycosides, flavonoids and phenols. The antioxidant activity and capacity test were carried out by conducting free radical of 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and Ferric reduction antioxidant plasma (FRAP) assays. Both assays showed S. tora leaf extract has higher antioxidant capacity than S. alata leaf extract. The efficacy of these leaf extracts were tested against skin pathogens through agar well diffusion method. S. alata extract showed an inhibition zone (1.15 – 1.59 mm) against Pseudomonas aeruginosa while S. tora extracts exhibited a strong antimicrobial activity against S. epidermidis (inhibition zone of 12 – 16.94 mm) followed by P. aeruginosa (inhibition zone of 1 – 1.59 mm). Nonetheless, no inhibition zone was observed for S. aureus by both leaf extracts. The phytochemicals and antioxidant constituents as well as inhibitory potential on skin pathogens possessed by S. alata and S. tora leave highlighted their potential utilization in the development of natural drugs or cosmetics to treat skin related diseases or infections.

scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIMICROBIAL ACTIVITIES OF BIS(CYCLOPENTADIENYL)TITANIUM(IV) COMPLEXES WITH SCHIFF BASES DERIVED FROM5-(SUBSTITUTED ARYL)-2-HYDRAZINO-1, 3, 4-OXADIAZOLE AND INDOLINE-2, 3-DIONE

2021 ◽  
Vol 9 (09) ◽  
pp. 900-909
Author(s):  
Anupama Srivastava ◽  
◽  
Shilpi Srivastava ◽  
Om. P. Pandey ◽  
Soumitra K. Sengupta ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Electrical Conductance ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Bacterial Strains ◽  
Monoclinic Crystal ◽  
Spectral Techniques ◽  
Concentration Method

Titanium(IV) complexes of type[(η5-C5H5)2TiCl(L)] have been synthesized by the reactions of bis(cyclopentadienyl)titanium(IV)dichloride with Schiff bases (LH) derived by the condensation of 5-(substituted aryl)-2-hydrazino-1,3,4-oxadiazole and indoline-2,3-dione in tetrahydrofuranin the presence oftriethylamine. All these complexes are soluble in PhNO2, DMF and DMSO.The complexes were characterized by elemental analyses, electrical conductance, magnetic susceptibility, UV-Vis, IR, 1H NMR, 13C NMR, XRD and SEM spectral techniques. Low molar conductance values indicate that they are non-electrolytes. The spectral data indicate5-coordinate geometry for the complexes.XRD pattern indicate that the complexes have monoclinic crystal system and particle sizes were found 49.36 nm (nano-size). In vitro antifungal activity of synthesized compounds was evaluated against fungi Aspergillusniger, Aspergillusflavus,ColletotrichumfalcatumandIn vitro antibacterial activity was determined by screening the compounds against gram negative (P. aeruginosa, S.typhi) and gram positive (S. aureus and B.subtilis) bacterial strains using minimum inhibition concentration method (MIC) by serial dilution technique. The titanocene(IV) complexes have higher antimicrobial effect than the parent Schiff bases.

scholarly journals Synthesis and Characterization of Cobalt(III) and Copper(II) Complexes of 2-((E)-(6-Fluorobenzo[d]thiazol-2-ylimino) methyl)-4-chlorophenol: DNA Binding and Nuclease Studies—SOD and Antimicrobial Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
K. Savithri ◽  
B. C. Vasantha Kumar ◽  
H. K. Vivek ◽  
H. D. Revanasiddappa
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Activities ◽  
Spectroscopic Studies ◽  
Docking Studies ◽  
Bacterial Strains ◽  
Spectral Techniques ◽  
Light Reduction ◽  
Drug Candidates ◽  
Ft Ir

A bidentate (N- and O-) imine-based ligand (L1) and its metal complexes of types [CuII(L1)2] (C1), [CuII(L1)(Phen)] (C2), [CoIII(L1)2] (C3), and [CoIII(L1)(Phen)] (C4) (L1 = 2-((E)-(6-fluorobenzo[d]thiazol-2-ylimino)methyl)-4-chlorophenol and phen = 1,10-phenanthroline) were synthesized as potential chemotherapeutic drug candidates. The prepared complexes were structurally characterized by spectral techniques (NMR, FT-IR, LC-MS, EPR, and electronic absorption), thermogravimetric analysis (TGA/DTA), magnetic moment, and CHNO elemental analysis. Spectroscopic studies suggested the distorted octahedral structure for all complexes. In vitro bioassay studies include binding and nuclease activities of the ligand and its complexes with target calf thymus- (CT-) DNA were carried out by employing UV-Vis, fluorescence spectroscopy, viscosity, and gel electrophoresis techniques. The extent of binding propensity was determined quantitatively by Kb and Ksv values which revealed a higher binding affinity for C2 and C4 as compared to C1 and C3. In addition, the scavenging superoxide anion free radical (O∙-2) activity of metal complexes was determined by nitroblue tetrazolium (NBT) light reduction assay. Molecular docking studies with DNA and SOD enzyme were also carried out on these compounds. The antimicrobial study has shown that all the compounds are potential antibacterial agents against Gram-negative bacterial strains and better antifungal agents with respect to standard drugs used.

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