scholarly journals SYNTHESIS, IN VITRO ANTIMICROBIAL ACTIVITY OF SCHIFF’S BASE, AZETIDINONES AND THIAZOLIDINONES

2016 ◽  
Vol 9 (1) ◽  
pp. 126
Author(s):  
Bhavnaben D. Mistry ◽  
Kishor R. Desai ◽  
Nigam J. Desai
Keyword(s):  
Acetyl Chloride ◽  
Thioglycolic Acid ◽  
Spectral Studies ◽  
Primary Aromatic Amine ◽  
Schiff’S Base ◽  
Mass Spectral ◽  
Microdilution Method ◽  
Good Antibacterial Activity ◽  
Antimicrobial Potency

Objective: The objective of the present study is to synthesize 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n]. The structure of all synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral studies. Methods: The titled compounds 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n] were synthesized by the reaction of N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene } substituted anilin [3a-n] with chloro acetyl chloride and thioglycolic acid respectively. Compounds N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene} substituted aniline [3a-n] were synthesized by the reaction of 3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-carbaldehyde [2] with primary aromatic amine in alcohol. All compounds were evaluated for their antimicrobial activity.Results: Compounds 3a,3b,3d,3j,3l,4d,4e,4j,4l,4m,5e,5g,5h,5n exhibited excellent to good antibacterial activity as compared to reference drugs.Conclusion: In summary, N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene } substituted anilin [3a-n], 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n] derivatives have been synthesized and characterized. In vitro antimicrobial testing of the compounds was carried out by microdilution Method. Amongst the synthesised compounds, many of them had proven their antimicrobial potency which varies from good to excellent.

scholarly journals Antimicrobial, Antifertility and Antiinflammatory Approach to Tetradentate Macrocyclic Complexes of Iron(II) and Manganese(II)

2002 ◽  
Vol 8 (6) ◽  
pp. 347-353 ◽  
Author(s):  
Ashu Chaudhary ◽  
D. P. Jaroli ◽  
R. V. Singh
Keyword(s):  
Molecular Weight ◽  
Reproductive Organs ◽  
Spectral Studies ◽  
Central Metal Atom ◽  
Central Metal ◽  
Testicular Sperm ◽  
Mass Spectral ◽  
Sperm Density ◽  
Elemental Analyses

Some antifertility inhibitors of 18 to 24-membered tetraazamacrocyclic complexes of iron(II) and manganese(II) have been synthesised by the template condensation using 1,3-phenylenediamine with malonic acid, succinic acid, glutaric acid and adipic acid. The reaction proceed smoothly to completion. The complexes were characterized by elemental analyses, molecular weight determinations, infrared, electronic, magnetic moment, mössbaur and mass spectral studies. The elemental analyses are consistent with the formation of the complexes [M(N4Ln)Cl2] (M = Fe(lI) or Mn(II)). All these complexes are stable and monomeric in nature as indicated by the molecular weight determinations. The spectral studies confirm the octahedral geometry around the central metal atom. The complexes have been screened in vitro against a number of fungi and bacteria to assess their growth inhibiting potential. The testicular sperm density and testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs have been examined and discussed.

scholarly journals Anti-Inflammatory Effects of 3-Formyl, 7-Flavonols Derivatives by Microwave Enhanced Chemistry Assisted - Vilsmeier Haack Synthesis

2019 ◽  
Vol 12 (04) ◽  
pp. 1779-1791
Author(s):  
M. Karpakavalli ◽  
A.Y. Sangilimuthu ◽  
A.Usha Raja Nanthini ◽  
G.Nagaraja Perumal ◽  
S. Mohan ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Population Increase ◽  
Spectral Studies ◽  
Dimethyl Formamide ◽  
Mass Spectral ◽  
Paw Oedema ◽  
Rf Values ◽  
Anti Inflammatory

In the modern medicines the novel and active molecules are essential to act against various diseases and increase the needs day by day due to population increase. In view of that, we attempt to make a variety of synthetic molecules against inflammation by a new and popular greener microwave assisted and faster method such as Microwave Enhanced Chemistry assisted Vilsmeier Haack Synthesis (MEC-VHS). In this paper, we report the synthesis of nitro- dinitro- and acetyl- derivatives of 3- formyl, 7-flavonols using MEC-VHS techniques against inflammation as anti-inflammatory agent. These derivatives were synthesized via pinkish formylation complex of dimethyl formamide and phosphorous oxychloride by microwave irradiation resulted as suspension by base. The re-crystallized products were characterized through Co-TLC, λmax, IR, HPTLC, 1HNMR, CHN analysis and mass spectral studies. The HPTLC finger print profiles obtained were of with a prominent single peak and with a matching Rf values compared to that obtained by an ordinary Co-TLC technique. All the synthesized compounds were screened for their anti-inflammatory activity by in vitro protein denaturation method and in vivo carrageenan induced paw oedema method and it was found that all the compounds excepting the un-substituted 3-formyl, 7-flavonols gave an equi- or more potent activity as compared to that of the standard.

scholarly journals Synthesis, Characterization, and Evaluation of Antimicrobial and Antifertility Efficacy of Heterobimetallic Complexes of Copper (II)

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Ashu Chaudhary ◽  
Anshul Singh
Keyword(s):  
Reproductive Organs ◽  
Male Rats ◽  
Spectral Studies ◽  
Molecular Weight Determination ◽  
Mass Spectral ◽  
Heterobimetallic Complexes ◽  
Group 4 ◽  
Electronic Spin ◽  
Substantial Decline

Heterobimetallic complexes of the copper with remarkable antimicrobial and antifertility action have been synthesized by the conventional method by reacting CuCl2 and o-phenylenediamine in the methanolic medium forming the mononuclear complex of the type CuC6H8N22Cl2 which was further treated with group 4 or 14 organometallic dichlorides (Ph2M′Cl2, Me2M′Cl2, and Cp2M′′Cl2) [M′ = Sn, Si, and M′′ = Ti, Zr] leading to formation of heterobimetallic complexes. All the synthesized complexes were characterized in the light of various physicochemical techniques like elemental analyses, conductivity measurements, molecular weight determination, electronic and infrared spectra, electronic spin resonance, X-ray, and mass spectral studies. The in vitro antibacterial activity of synthesized complexes against Escherichia coli and Staphylococcus aureus was tested to evaluate their inhibiting activities. The antifungal activities of mono- and heterobimetallic complexes were studied by screening the compounds against Fusarium oxysporum and Alternaria alternata. These complexes were then investigated to reveal their effect on the reproductive organs of male rats. The treatment has shown substantial decline in the sperm motility and density signifying the imperious antifertility activity.

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 New oxadiazole derivatives of isonicotinohydrazide in the search for antimicrobial agents: Synthesis and in vitro evaluation

2012 ◽  
Vol 77 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Manav Malhotra ◽  
Mohit Sanduja ◽  
Abdul Samad ◽  
Aakash Deep
Keyword(s):  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Spectral Studies ◽  
Dilution Method ◽  
Mass Spectral ◽  
Oxadiazole Derivatives ◽  
Derivatives Of ◽  
And Staphylococcus Aureus

Structural modification of the front line antitubercular drug isoniazid provide a lipophilic adaptations of the drug in which hydrazide moiety of isoniazid is replaced by 1,3,4-oxadiazole heterocycles to eliminate in-vivo acetylation by arylamine N-acetyltransferase which results to form inactive acetylated drug. In the present study a series of sixteen oxadiazole derivatives were synthesized and characterized by (IR, 1H NMR, 13C NMR and Mass spectral) studies. All the synthesized compounds were evaluated for their antimicrobial activity by broth dilution method against two Gram positive strains (Bacillus subtilis and Staphylococcus aureus), two Gram negative strains (Pseudomonas aeruginosa and Escherichia coli) and fungal strain (Candida albicans and Aspergillus niger). The minimum inhibitory concentration of the compounds was in the range of 1.56-50 ?g ml-1 against bacterial and fungal strain. The results revealed that all synthesized compounds have a significant biological activity against the tested microorganisms. Among the synthesized derivatives 4g, 4h, 4m and 4p were found to be most effective antimicrobial compounds.

scholarly journals Synthesis, antimicrobial and antimalarial activityof1, 4-benzothiazepine and pyrazolinederivatives incorporating carbazolemoiety

2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
13C Nmr ◽  
Antimalarial Activity ◽  
Positive Control ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Ft Ir

A series of carbazole-based 1,4-benzothiazepine and pyrazoline derivatives were synthesized and the structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and mass spectral studies. All new derivatives 4(a-f) and 5(a-e) were screened for their in vitro antimicrobial activity, and also for their antimalarial activity. Compounds 4a, 4b, 4d, 5a, 5b and 5c exhibited promising antimicrobial and antimalarial activities as compared to positive control. Notably, compounds 4a, 4b and 4d showed excellent antifungal activity against Penicillium sp. comparable to that of a standard drug.

Bioefficacy of Mikania micrantha H.B.K. against Water-Borne Bacterial Pathogens

2017 ◽  
Vol 5 (1) ◽  
pp. 52-57
Author(s):  
Awadhesh Kumar ◽  
◽  
Nagaraj Hegde ◽  
Keyword(s):  
Plant Secondary Metabolites ◽  
Mikania Micrantha ◽  
E Coli ◽  
Microdilution Method ◽  
Good Antibacterial Activity ◽  
Ic50 Value ◽  
Broth Microdilution Method ◽  
Thermo Stability ◽  
Microbial Attack

The plant secondary metabolites play a very important role during the microbial attack. These metabolites (essential oils/ alkaloids/ glycosides/ tannins etc.) can be extracted from plant and many of these plant products can be used as a potential source for new antibacterial agents. In thepresent investigation, the extract extracted from dried leaves of Mikania micrantha by using Soxlet apparatus. The efficacy of extract was analyzed by broth microdilution method of CLSI against the E. coli, K. pneumoniae, P. vulgaris and S. dysenteriae in in-vitro condition. The result showed the minimum inhibitory concentration 0.317mg/ ml against E. coli; 0.429mg/ ml against K. pneumoniae; 1.16mg/ml against P. vulgaris and 0.437mg/ ml against S. dysenteriae; however, IC50 value was recorded as 0.162, 0.211, 0.670 and 0.214, respectively. The finding showed that the extract of M. micrantha having a good antibacterial activity. Its toxicity persisted heavy inoculums density, thermo stability and long shelf life.

scholarly journals DESIGN, SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES CONTAINING INDOL- THIAZOLYL- THIAZOLIDINONE DERIVATIVES

2018 ◽  
Vol 11 (3) ◽  
pp. 113 ◽  
Author(s):  
Prabhakar Walmik ◽  
Basavaraj S Naraboli ◽  
Swathi B ◽  
Somashekhar Ghanti
Keyword(s):  
Analytical Data ◽  
Biologically Active ◽  
Design Synthesis ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Microdilution Method ◽  
13C Nuclear Magnetic Resonance ◽  
Broth Microdilution Method ◽  
Antibacterial And Antifungal

 Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7- trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7- trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c).Methods: All the newly synthesized compounds were characterized by infrared, 1H, 13C nuclear magnetic resonance and mass spectral data and elemental analysis and evaluated for in vitro antimicrobial activity.Results: Novel compounds N-((5-Substituted-2-phenyl-1H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted- 2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethyl benzo[d]thiazol-2-yl)thiazolidin-4-one (6a-c) have been made and characterized using spectral and analytical data. The results of antibacterial and antifungal activities showed that some of the synthesized compounds exhibited promising activities.Conclusion: All the newly synthesized compounds were carried out by the broth microdilution method (NCCLS. 2002) in a DMF concentration of 500, 250, 125, and 62.5 μg/ml. Gentamycin and fluconazole are used as reference standards for antibacterial and antifungal activity, respectively. The final results revealed that compounds 4b, 5b, and 6b exhibited potent antimicrobial activity when compared to the standard drugs. 

scholarly journals Cu(II), Ni(II), and Zn(II) Complexes of Salan-Type Ligand Containing Ester Groups: Synthesis, Characterization, Electrochemical Properties, andIn VitroBiological Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
P. Jeslin Kanaga Inba ◽  
B. Annaraj ◽  
S. Thalamuthu ◽  
M. A. Neelakantan
Keyword(s):  
Cyclic Voltammetry ◽  
Magnetic Moments ◽  
Spectral Studies ◽  
Planar Geometry ◽  
Binding Modes ◽  
Tetrahedral Geometry ◽  
Mass Spectral ◽  
Displacement Assay ◽  
Voltammetry Methods

A salen ligand on reduction and N-alkylation affords a novel [N2O2] chelating ligand containing ester groups [L = diethyl-2,2′-(propane-1,3-diylbis((2-hydroxy-3-methoxy benzyl)azanediyl))diacetate]. The purity of the ligand was confirmed by NMR and HPLC chromatograms. Its Cu(II), Ni(II), and Zn(II) complexes were synthesized and characterized by a combination of elemental analysis, IR, NMR, UV-Vis, and mass spectral data, and thermogravimetric analysis (TG/DTA). The magnetic moments, UV-Vis, and EPR spectral studies support square planar geometry around the Cu(II) and Ni(II) ions. A tetrahedral geometry is observed in four-coordinate zinc with bulky N-alkylated salan ligand. The redox properties of the copper complex were examined in DMSO by cyclic voltammetry. The voltammograms show quasireversible process. The interaction of metal complexes with CT DNA was investigated by UV-Vis absorption titration, ethidium bromide displacement assay, cyclic voltammetry methods, and agarose gel electrophoresis. The apparent binding constant values suggest moderate intercalative binding modes between the complexes and DNA. Thein vitroantioxidant and antimicrobial potentials of the synthesized compounds were also determined.

scholarly journals Synthesis, Spectral Studies and Antimicrobial Activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives

2017 ◽  
Vol 5 (04) ◽  
pp. 34-38
Author(s):  
Monika Gupta ◽  
Baljeet Kaur ◽  
Shailender Pratap Singh ◽  
Vivek Kumar Gupta
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Good Antibacterial Activity ◽  
Thiadiazole Ring ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Thiadiazole is a heterocyclic compound containg both two nitrogen atom and one sulfur atom as a part of the aromatic five-membered ring. The imidazo [2,1-b]-1,3,4-thiadiazole ring system is the core skeleton of well known immunomodulator levamisole. The synthesis and antimicrobial activity of nine 6-Phenyl-2- substituted imidazo [2,1-b]-1,3,4-thiadiazole derivatives were reported against Gram +ve bacteria Bacillius subtilis (MTCC 121), Staphyloccus aureus (MTCC 87), Gram –ve bacteria Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 40), and fungal strains Candida albicans (MTCC 183), Fusarium solani (MTCC 2935), Fusarium oxyporium (MTCC 2840). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The synthesized compound (6) and (5b) had moderate antibacterial activity especially with Gram negative Escherichia coli (MTCC 40) where (5a) and (5f) had good antibacterial activity. The structures of the synthesized compounds were established by IR, NMR and Mass spectral studies.

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