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

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.

2002 ◽  
Vol 8 (6) ◽  
pp. 347-353 ◽  
Author(s):  
Ashu Chaudhary ◽  
D. P. Jaroli ◽  
R. V. Singh

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.


2019 ◽  
Vol 12 (04) ◽  
pp. 1779-1791
Author(s):  
M. Karpakavalli ◽  
A.Y. Sangilimuthu ◽  
A.Usha Raja Nanthini ◽  
G.Nagaraja Perumal ◽  
S. Mohan ◽  
...  

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.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik

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.


2012 ◽  
Vol 77 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Manav Malhotra ◽  
Mohit Sanduja ◽  
Abdul Samad ◽  
Aakash Deep

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.


2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke

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.


Author(s):  
Bhavnaben D. Mistry ◽  
Kishor R. Desai ◽  
Nigam J. Desai

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.


2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
P. Jeslin Kanaga Inba ◽  
B. Annaraj ◽  
S. Thalamuthu ◽  
M. A. Neelakantan

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.


2020 ◽  
Vol 5 (4) ◽  
pp. 295-300
Author(s):  
Yogesh J. Sanghani ◽  
Suresh B. Koradiya ◽  
Krushnakumar J. Jilariya

In this work, pyrazole based oxothiazolidine hybrids, 4-{4-[2-(1- phenyl-3-(substituted)phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3- yl]-phenyl}-morpholin-3-one (11a-l) were synthesized using molecular hybridization approach through Vilsmeier-Haack reaction. The titled compounds 11a-l were characterized by elemental analysis, IR, 1H NMR and mass spectral studies. The antibacterial activity of 11a-l was evaluated in vitro by agar cup plate method against B. cocous, B. subtillis, E. coli and P. vulgaris. The antifungal activity of compounds 11a-l was evaluated in vitro by agar based disk diffusion method against A. niger. The results of antibacterial and antifungal evaluation were reported in terms of zone of inhibition measured in mm. The synthesized compounds 11a-l exhibited moderate to good antibacterial and antifungal potential. Compound 4-{4-[2-(1-phenyl-3-(2-methoxyphenyl) phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3-yl]-phenyl}- morpholin-3-one (11h) emerged as a most potent antimicrobial agent displaying zone of inhibition 21, 20, 21, 24 and 20 mm against B. cocous, B. subtillis, E. coli, P. vulgaris and A. niger, respectively.


2006 ◽  
Vol 71 (6) ◽  
pp. 587-591 ◽  
Author(s):  
H.G. Sangani ◽  
K.B. Bhimani ◽  
R.C. Khunt ◽  
A.R. Parikh

Barbitones (3) were synthesised by the condensation of chalcones (2) with barbituric acid. The structure of the synthesized compounds were assigned on the basis of elemental analyses, IR, NMR and mass spectral studies. All the products were evaluated for their in vitro antimicrobial activity against various strains of bacteria and fungi.


2021 ◽  
Vol 6 (2) ◽  
pp. 116-120
Author(s):  
Raj Bahadur Singh ◽  
Krishna Srivastava ◽  
Ram Prakash Tiwari ◽  
Jyoti Srivastava

The present work reports the synthesis of 4-(1-(substituted phenyl)-1H-naphtho[1,2-e][1,3]oxazin- 2(3H)-yl)-1-thia-4-azaspiro-[4.5]-decan-3-one IV(a-h) by 4-(((substituted phenyl)(2-hydroxynaphthalen- 1-yl) ethyl)amino)-1-thia-4-azaspiro[4.5]decan-3-one with formaldehyde in acetonitrile, containing a spiro ring obtained from the reaction of cyclohexylidene hydrazine and thioglycollic acid in DMF (cyclohexanone reacts with hydrazine hydrate in pyridine). The structures of the synthesized compounds have been established on the basis of elemental analysis, UV-vis absorption spectroscopy, IR, 1H NMR and mass spectral studies. The in vitro antimicrobial screening of all novel compounds was done against S. aureus, E. coli, P. aeruginosa and B. subtilis. The activity of compounds IVb, IVc, IVe and IVf compounds showed moderate to good activity against the tested microbes.


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