scholarly journals Microwave Assisted Synthesis of Novel Imidazolopyridinyl Indoles as Potent Antioxidant and Antimicrobial Agents

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Jaiprakash S. Biradar ◽  
Parveen Rajesab ◽  
Sasidhar B. Somappa
Keyword(s):  
Antimicrobial Agents ◽  
Analytical Data ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
The Novel ◽  
Design Synthesis ◽  
Mass Spectral ◽  
H Nmr ◽  
Total Antioxidant ◽  
Indole Analogues

We describe herein the design, synthesis, and pharmacological evaluation of novel series of imidazolopyridinyl indole analogues as potent antioxidants and antimicrobials. These novel compounds (3a–i) were synthesized by reacting 3,5-disubstituted-indole-2-carboxylic acid (1a–i) with 2,3-diamino pyridine (2) in excellent yield. The novel products were confirmed by their IR,1H NMR,13C NMR, mass spectral, and analytical data. These compounds were screened for their antioxidant and antimicrobial activities. Among the compounds tested,3a–dshowed the highest total antioxidant capacity, scavenging, and antimicrobial activities. Compounds3c-dand3g-hhave shown excellent ferric reducing activity.

Design and synthesis of novel thiopheno-4-thiazolidinylindoles as potent antioxidant and antimicrobial agents

2014 ◽  
Vol 68 (3) ◽  
Author(s):  
Jaiprakash Biradar ◽  
Parveen Rajesab ◽  
B. Sasidhar
Keyword(s):  
Antimicrobial Agents ◽  
Analytical Data ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Mercaptoacetic Acid ◽  
Antioxidant Power ◽  
Mass Spectral ◽  
Design And Synthesis ◽  
High Yields

AbstractA novel and convenient synthesis of thiopheno-4-thiazolidinyl indole analogues is presented (IVa-IVi), with the aim of obtaining biologically active compounds. 3,5-disubstituted indol-2-carboxyhydrazides (Ia-If) were allowed to react with 3-acetyl-2,5-dichlorothiophene (II) to yield the corresponding 3,5-disubstituted indol-2-carbohydrazides (IIIa-IIIf). The pre-formed indolecarbohydrazides (IIIa-IIIf) were allowed to react with 2-mercaptoacetic acid or 2-mercaptopropanoic acid to produce thiopheno-4-thiazolidinylindoles (IVa-IVi). This reaction protocol affords a simple, eco-friendly, non-hazardous, easier preparation and high yields. The antioxidant (free radical scavenging, total antioxidant capacity and ferric-reducing antioxidant power) and antimicrobial activities of the synthesised compounds were evaluated. The structures and purity of the products were confirmed by their IR, 1H NMR, 13C NMR and mass spectral and analytical data. Most of the compounds tested showed very significant scavenging, antioxidant and antimicrobial activities. Compounds containing electron donor group (CH3) at the fifth position of indole exhibit an excellent ferric-reducing activity. The present study suggests that compounds IIIa-IIIb, IIIf, IVa-IVc, IVf-IVi, may serve as promising lead scaffolds for antioxidant and antimicrobial agents.

scholarly journals A Mini Library of Novel Triazolothiadiazepinylindole Analogues: Synthesis, Antioxidant and Antimicrobial Evaluations

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Jaiprakash Sharanappa Biradar ◽  
Parveen Rajesab ◽  
Naveen Jaiprakash Biradar ◽  
Sasidhar Balappa Somappa
Keyword(s):  
Radical Scavenging Activity ◽  
Analytical Data ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Free Radical Scavenging ◽  
Scavenging Activity ◽  
H Nmr ◽  
Total Antioxidant ◽  
Antioxidant And Antimicrobial Activities ◽  
Antimicrobial Potency

A new series of novel triazolothiadiazepinylindole analogues were synthesized with an aim to examine possible antioxidant and antimicrobial activities. The titled compounds (3a–z) were obtained in good yield by reacting 5-(5-substituted-3-phenyl-1H-indol-2-yl)-4-amino-4H-1,2,4-triazole-3-thiols1a–cwith 3-(2,5-disubstituted-1H-indol-3-yl)-1(4-substituted phenyl)prop-2-en-1-ones2a–i. All the newly synthesized compounds were characterized by IR,1H NMR, mass spectroscopic and analytical data. The synthesized analogues were tested for antioxidant and antimicrobial potency. Among the tested compounds3a–cand3j–lhave shown very promising free radical scavenging activity and total antioxidant capacity. Compounds3d–f,3m–o, and3s–zhave shown excellent ferric reducing antioxidant activity. An outstanding antimicrobial activity is observed with compounds3a–cand3j–l.

scholarly journals Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Rizk E. Khidre ◽  
Ibrahim Ali M. Radini
Keyword(s):  
Antimicrobial Agents ◽  
Docking Simulation ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
The Novel ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
In Silico Molecular Docking

AbstractA novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline, respectively. The potential DNA gyrase inhibitory activity was examined using in silico molecular docking simulation. The novel thiazoles exhibit dock score values between − 6.4 and − 9.2 kcal/mol and they were screened for their antimicrobial activities. Compound 13a shown good antibacterial activities with MIC ranged from 93.7–46.9 μg/mL, in addition, it shown good antifungal activities with MIC ranged from 7.8 and 5.8 μg/mL.

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

Fluorinated s-Triazinyl Piperazines as Antimicrobial Agents

2011 ◽  
Vol 66 (7-8) ◽  
pp. 345-352 ◽  
Author(s):  
Rahul V. Patel ◽  
Premlata Kumari ◽  
Kishor H. Chikhalia
Keyword(s):  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Salmonella Typhi ◽  
The Novel ◽  
Proteus Vulgaris ◽  
Aspergillus Clavatus ◽  
H Nmr ◽  
Chemical Structures ◽  
Triazine Derivatives ◽  
C Nmr

A series of 1,3,5-triazine derivatives that contain 4-amino-2-trifl uoromethyl-benzonitrile, 8-hydroxyquinoline, and different piperazines as substituents at the carbon atoms of the triazine ring have been synthesized by a simple and efficient synthetic protocol. The chemical structures of the compounds were elucidated with the aid of IR, 1H NMR and 13C NMR spectroscopy, and elemental analysis. The antimicrobial activity of the compounds was tested against seven bacteria (Staphylococcus aureus MTCC 96, Bacillus cereus MTCC 619, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 741, Klebsiella pneumoniae MTCC 109, Salmonella typhi MTCC 733, Proteus vulgaris MTCC 1771) and four fungi (Aspergillus niger MTCC 282, Aspergillus fumigatus MTCC 343, Aspergillus clavatus MTCC 1323, Candida albicans MTCC 183). The results indicate that some of the novel s-triazines have noteworthy activity in minimum inhibitory concentration as well as agar diffusion tests.

scholarly journals Synthesis, Spectral and Microbial Studies of Some Novel Schiff Base Derivatives of 4-Methylpyridin-2-amine

2009 ◽  
Vol 6 (4) ◽  
pp. 1205-1210 ◽  
Author(s):  
J. J. Vora ◽  
S. B. Vasava ◽  
K. C. Parmar ◽  
S. K. Chauhan ◽  
S. S. Sharma
Keyword(s):  
Schiff Base ◽  
Antimicrobial Activities ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Acid Catalyzed ◽  
Derivatives Of ◽  
Broth Dilution

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.

scholarly journals Synthesis, Characterization, and Thermal and Antimicrobial Activities of Some Novel Organotin(IV): Purine Base Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik
Keyword(s):  
Antimicrobial Agents ◽  
Rhizopus Oryzae ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Purine Base ◽  
Mass Spectral ◽  
E Coli ◽  
Kinetic And Thermodynamic Parameters ◽  
C Nmr

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.

scholarly journals Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives

2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Microwave Assisted Synthesis ◽  
Mass Spectral Data ◽  
Pyrimidine Derivatives ◽  
Plate Method ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
New Compounds

The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidines 1a-j are compared with those of known chosen standard drugs, viz. ampicillin, chloramphenicol, ciprofloxacin, norfloxacin and griseofulvin. .

scholarly journals Design, Synthesis, Antibacterial and Antifungal Activity of Novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones

2012 ◽  
Vol 9 (3) ◽  
pp. 1481-1489
Author(s):  
Anisetti Ravinder Nath ◽  
Malladi Srinivas Reddy
Keyword(s):  
Antifungal Activity ◽  
Knoevenagel Condensation ◽  
Catalytic Amount ◽  
The Novel ◽  
Plate Method ◽  
Design Synthesis ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal

The novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones (4a-j) analogs were synthesized by Knoevenagel condensation of a solution of 2-methyl-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4-dihydro-4-quinazolinone (3) with aromatic aldehyde in presence of catalytic amount of piperidine. Compounds (4a-j) showed significant biological activity against all the standard strains. All the synthesized compounds were characterized on the basis of their IR,1H NMR, MASS spectroscopic data and elemental analyses. All the compounds have been tested for antimicrobial and antifungal activity by the cup-plate method.

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