scholarly journals Synthesis, Characterization, Semiempirical and Biological Activities of Organotin(IV) Carboxylates with 4-Piperidinecarboxylic Acid

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Shabbir Hussain ◽  
Saqib Ali ◽  
Saira Shahzadi ◽  
Saroj K. Sharma ◽  
Kushal Qanungo ◽  
...  

Organotin (IV) carboxylates with the general formulae R2Sn(Cl)L [R = Me (1),n-Bu (2), Ph (3)] and R3SnL [R = Me (4), Ph (5)] have been synthesized by the reaction of 4-piperidinecarboxylic acid (HL) with KOH and R2SnCl2(R = Me,n-Bu, Ph)/R3SnCl (R = Me, Ph) in methanol under stirring conditions. The metal ligand binding site, structure, and stability of complexes have been verified by FT-IR, (1H,13C) NMR, EI-MS technique, and semiempirical study. The FT-IR data indicate the bidentate chelating mode of the carboxylate ligand which is also confirmed by semiempirical study. In solution state, five and four coordinated geometry around tin was confirmed by NMR spectroscopy. The EI-MS data agreed well with the molecular structure of the complexes. Thermodynamic parameters and molecular descriptors were calculated by using semiempirical PM3 method. HOMO-LUMO calculations show that chlorodiorganotin complexes are more susceptible to nucleophilic attack as compared to triorganotin complexes. Computed negative heat of formation indicates that complexes1–4are thermodynamically stable. The organotin(IV) carboxylates displayed powerful antimicrobial activities against various strains of bacteria and fungi and their minimal inhibitory concentration were also evaluated. The complexes exhibited comparatively higher hemolytic activity as compared to free ligand.

2019 ◽  
Vol 31 (10) ◽  
pp. 2331-2336 ◽  
Author(s):  
Manoj Kumar ◽  
Anita Rani ◽  
Hardeep Singh Tuli ◽  
Rajshree Khare ◽  
Vinit Parkash

This report describes the synthesis and exploration of novel Schiff base ligand in the form of a polymer (heptamer) which was prepared by reaction between 3,4-diacetyl-2,5-hexanedione and hydrazine hydrate in ethanol. On further reaction of Schiff base with transition metals ions (Co and Cu) leads to formation of its transition metal complexes. The structural identification of Schiff base ligand and its transition metal complexes were characterized by classical structural techniques like FT-IR, NMR and mass spectra. The free ligand and its transition metal complexes have been screened for in vitro biological activities against various strains of bacteria and fungi. The prepared Schiff base and its metal complexes were also screened for antiangiogenic activity. The results have shown the remarkable antimicrobial and antiangiogenic activities of the Schiff base and its metal complexes.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3170
Author(s):  
Wafaa M. Elkady ◽  
Mariam H. Gonaid ◽  
Miriam F. Yousif ◽  
Mahmoud El-Sayed ◽  
Hind A. N. Omar

Active components from natural sources are the current focus in most pharmacological research to provide new therapeutic agents for clinical use. Essential oils from the Pinus species have been traditionally used in medicine. This study aimed to investigate the chemical profile of two Pinus species, Pinus halepensis L. and Pinus pinea Mill, from different altitudes in Libya and study the effect of environmental conditions on the biological activities of essential oils. A clevenger apparatus was used to prepare the essential oils by hydrodistillation. Analyses were done using GC/MS. Anthelmintic and antimicrobial activities were tested against the earthworm Allolobophora caliginosa, gram-positive bacteria, gram-negative bacteria, and fungi. Different chemical profiles were observed among all tested essential oils, and terpenes were the most dominant class. All studied essential oils from the Pinus species exhibited a remarkable anthelmintic activity compared to the standard piperazine citrate drug. Pinus halepensis from both altitudes showed broad-spectrum antimicrobial activity against all tested microorganisms, while Pinus pinea was effective against only Escherichia coli. From these findings, one can conclude that there are variations between studied species. The essential oil compositions are affected by environmental factors, which consequently affect the anthelmintic and antimicrobial activity.


2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).


2012 ◽  
Vol 7 (2) ◽  
pp. 327-333 ◽  
Author(s):  
Pavle Mašković ◽  
Jelena Maksimović ◽  
Vuk Maksimović ◽  
Jelena Blagojević ◽  
Mladen Vujošević ◽  
...  

AbstractThe objective of this study was to evaluate the efficacy of the ethanolic extract of endemic plant Halacsya sendtneri in inhibiting the growing of the test fungi and bacteria as well as to determine its genotoxic potential and toxicity using the Allium anaphase-telophase assay. Minimum inhibitory concentrations (MIC) were determined for 15 indicator strains of pathogens, representing both bacteria and fungi. The highest susceptibility to the ethanolic extract of H.sendtneri was exhibited by Pseudomonas glycinea (FSB4), (MIC=0.09 mg/ml) among the bacteria, and by Phialophora fastigiata (FSB81), (MIC=1.95 mg/ml) among the fungi. The composition of H. sendtneri extracts was also determined using HPLC analysis. Rosmarinic acid was found to be the dominant phenolic compound. The Allium anaphase-telophase genotoxicity assay revealed that the ethanolic extract of H. sendtneri at concentrations of 31.5 mg/l and below does not produce toxic or genotoxic effects. This is the first report of chemical constituents, genotoxic and antimicrobial activities of the endemic species, H. sendtneri.


Author(s):  
Indu Raj ◽  
Dr.Smt. Manjul Shrivastava

In view of the fact that a large number of derivatives of benzoxazole have been found toexhibit a wide variety of antimicrobial activities. Heterocyclic compounds play an importantrole in medicinal chemistry and exhibit wide range of biological activities in pharmaceuticalchemistry. Complexes of 2-aminobenzoxazole (L) with chloride of iron (II), was synthesized.The molar ratio metal: ligand in the reaction of the complex formation was 1:2. It should benoticed, that the reaction of all the metal salts yielded bis (ligand) complex of the generalformula M (L) 2(CL) 2. The complex was characterized by elemental analysis, melting point,FT-IR, 1H NMR, spectral data. The antifungal activity against different fungai, A.niger,A.flavus, Fusarium oxysporum, paecilomyces variotii, C.albicans.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 3124-3136
Author(s):  
Rajeswari S ◽  
Harindran Suhana ◽  
Kalaivizhi R

1-((dicyclohexylamino)(phenyl)methyl) pyrrolidine-2,5-dione (SDB) has been synthesized as a result of succinimide, benzaldehyde and dicyclohexylamine Mannich base condensation and its CoII, NiII and CuII complexes were prepared. The structure of the Mannich Base ligand (SDB) was elucidated on the basis of FT-IR, 1H NMR, 13C NMR and Mass spectral studies. The monomeric and non-electrolytic nature of the metal complexes is evidenced by their magnetic susceptibility and low conductance data studies. Spectral tests, mainly FT-IR studies as well as elemental analysis, were carried out to verify the structures of the newly synthesized compounds. All the metal complexes possess a six-coordinate geometry. The synthesized ligand and its metal complexes have been tested against Gram-positive strains (Staphylococcus aureus and Micrococcus luteus), Gram-negative strains (Escherichia coli and Pseudomonas aeruginosa) and fungal strains (Aspergillus niger and Aspergillus fumigates) for their in vitro anti-bacterial and anti-fungal activities. Preliminary antimicrobial studies of the ligand and their metal complexes have also been carried out in order to understand the toxic effect of ligands and metal complexes against the selective microbes. The results showed that the metal chelates of the ligands showed higher antimicrobial activities than the free ligand SDB and CoII  complexes possess higher activity than the other metal complexes. 


Author(s):  
G. M. Turky ◽  
Esmat Hamzawy ◽  
Gehan Bassyouny ◽  
Sayed Kenawy ◽  
Abeer A. Abd El-Aty

Abstract Synthesis and characterization of biocomposite materials of hydroxyapatite (HA) and yttrium oxide (Y2O3) were investigated. HA nanoparticles powder was obtained from mussel shells via a wet chemical precipitation routine. HA powder was doped with 1 and 2 wt% of Y2O3 . For microstructural examination, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM) coupled with energy dispersive X-rays (EDX) were used. In addition, the dielectric and electrical properties and antimicrobial activities were investigated. XRD patterns reveal the crystallization of the oxyapatite. The peak intensities of pristine HA are inferior compared to the yttrium containing HA composites, thus suggesting that the addition of yttrium promotes the crystallization of HA due to the variance in their ionic radii. FT-IR shows a variation in the phosphate wavenumber, indicating the integration of yttrium into the HA matrix. SEM reveals nanorod- or worm-like crystals arose in clusters. With increasing Y2O3, from 1 to 2 wt%, the DC conductivity reduces from 16 to 9.3 nS/cm, which confirms that high amounts of Y3+ substitute Ca2+ in the HA matrix. In the high-frequency range, the AC conductivity linearly increases with increasing frequency following the universal power law. Further, antimicrobial activity results showed that the addition of yttrium in HA improves the antimicrobial effects against pathogenic bacteria and fungi. Additional research is needed to investigate the doping concentration of yttrium ions, and an anticipated property could be comprehended for several forthcoming biomedical applications


2021 ◽  
Vol 42 (1) ◽  
pp. 6-15
Author(s):  
Prem Shankar Deo ◽  
Rhambus Rawat ◽  
Bhushan Shakya

Triazole nucleus has drawn much attention since the last decade because of its various potent biological activities. The pharmacological application of triazoles has been widely recognized and well documented. Schiff and Mannich bases are both considered as bioactive compounds, however, there are not much of documentation about the Mannich bases as their study has begun lately. The main aim of this study was to synthesize new Mannich bases from Schiff base bearing 1,2,4-triazole nucleus to access their antimicrobial activities. The newly synthesized compounds 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a & 5b) were characterized by spectral techniques like UV, FT-IR, and NMR. Mannich bases were tested against various bacterial (gm +ve and gm –ve) as well as fungal strains. The synthesized Mannich bases showed good to moderate activities against the tested bacterial and fungal strains.


2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Ahmed A. Al-Amiery ◽  
Yasmien K. Al-Majedy ◽  
Haziem Abdulreazak ◽  
Hussain Abood

Problem Statement. In Iraq like most third world countries, attempts discovered new antibiotic drugs derived from thiosemicarbazide and its metal complexes and developed the branch of applied in organic chemistry.Approach. New (Z)-2-(pyrrolidin-2-ylidene)hydrazinecarbothioamide (L) was synthesized in a good yield by the reaction of pyrrolidone with thiosemicarbazide. Co(II), Ni(II), and Cu(II) complexes of (L) were prepared and characterized by FT-IR, UV/visible spectra,1HNMR, and CHN analyses. Moreover, charge, bond length, bond angle, twist angle, heat of formation, and steric energy were calculated by using of the ChemOffice program, and the DFT calculations for the complexes were done. The free ligand and its metal complexes were testedin vitroagainst several microorganisms (Staphylococcus aurous,E. coli,Proteus vulgaris,Pseudomonas, andKlebsiella pneumoniae) to assess their antimicrobial properties.Results. The study shows that these complexes have octahedral geometry; in addition, it has high activity against tested bacteria.Conclusion/Recommendations. Based on the reported results, it may be concluded that ligand acts as bidentate, neutral ligand, coordinating through one of the nitrogen and sulfur atoms.


2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.


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