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1.
Environ Monit Assess ; 196(8): 710, 2024 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-38976119

RESUMO

Industrial dye degradation involves several processes by which dyes are broken down, ideally into innocuous products. Methylene blue (MB) is one of the most commonly employed dyes in the textile industry and is released into water in routine industry processes. These discharges lead to creating a nocuous nature for humans and animals. Drugs are also discharged into water bodies from various pharmaceutical industries. In these two contexts, in the present work, the green synthesis of calcium-doped zinc oxide nanoparticles (Ca-doped ZnO NPs) is achieved using the aqueous peel extract of Citrus limetta by the solution combustion technique. The structural, morphological, and optical properties of the synthesized Ca-doped ZnO NPs are investigated using XRD, FTIR, SEM, EDX, and UV-visible spectroscopy. The prepared NPs were subjected to photocatalytic degradation of MB dye under visible-light illumination, which shows ~ 95% dye degradation. The synthesized Ca-doped ZnO NPs were also employed to adsorb tinidazole (TDZ), a nitroimidazole antibiotic, from water samples. An excellent adsorptive capacity of the NPs was observed for selectively adsorbing the TDZ ~ 96.2%. The drug TDZ was found to have pseudo-second-order kinetics. The catalyst recycling proved its repeatability; removal of the dye reached up to 92% after three successive usages. Therefore, using waste Citrus limetta peel extract, the multifunctional Ca-doped ZnO NPs were synthesized, which maintained effective adsorption potential and photocatalytic abilities and could be used as an effective material for environmental remediation.


Assuntos
Azul de Metileno , Tinidazol , Poluentes Químicos da Água , Óxido de Zinco , Óxido de Zinco/química , Poluentes Químicos da Água/química , Poluentes Químicos da Água/análise , Azul de Metileno/química , Tinidazol/química , Adsorção , Corantes/química , Cálcio/química , Cálcio/análise , Eliminação de Resíduos Líquidos/métodos , Citrus/química , Nanopartículas Metálicas/química , Nanopartículas/química
2.
Spectrochim Acta A Mol Biomol Spectrosc ; 291: 122297, 2023 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-36634496

RESUMO

Zinc oxide (ZnO) is one of the semiconductor materials with unique antimicrobial properties towards various microorganisms. In this article, pure and Na doped ZnO nanopowders were synthesized by easiest and cost-effective co-precipitation process. X-ray diffraction (XRD),Fourier transform infrared spectroscopy(FT-IR), ultraviolet - visible (UV - Vis) spectroscopy, scanning electron microscopy(SEM), and Energy dispersive X-ray analysis (EDAX) techniques were used to characterize the particle size, surface morphology and chemical composition of prepared materials. The XRD analysis revealed that the samples exhibiting hexagonal wurtzite crystal structure with high crystallinity and the average crystallite size values increased from 23.51 to 28.118 nm. The UV - Vis spectroscopy results exposed that the bandgap energy (Eg) of the samples with the values in the range of 3.068-3.301 eV. The SEM micrographs showed that the morphology of the of synthesized particles are hexagonal and spherical in nanometric size. The EDX spectra confirmed the elemental composition of Na, Zn and O in the crystal lattice and FTIR spectroscopic data proved the formation of functional groups and the presence of chemical bonding at the ZnO interface.Antibacterial activity of pure and Na doped Zinc oxide nanoparticles against Gram-negative pathogenssuch as Escherichia coli, Pseudomonas aeruginosa & Klebsiella pneumoniae and Gram-positive pathogens such as Staphylococcus aureus reveal that the zone of inhibition increases with increasing Na concentration. The antifungal activity against Aspergillus and Candida was investigated.These results demonstrated that the pure and Na doped ZnO samples exhibit enhanced antibacterial and antifungal activity with increasing particle sizein presence of visible light and they could be used as good antibacterial as well as antifungal agents.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Óxido de Zinco , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Antifúngicos/farmacologia , Antifúngicos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Sódio , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Difração de Raios X
3.
Eur J Med Chem ; 45(11): 5331-6, 2010 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-20855133

RESUMO

Recently we have reported the effect of (S)-6-aryl urea/thiourea substituted-2-amino-4,5,6,7-tetrahydrobenzo[d]thiazole derivatives as potent anti-leukemic agents. To elucidate further the Structure Activity Relationship (SAR) studies on the anti-leukemic activity of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzo[d]thiazole moiety, a series of 2-arlycarboxamide substituted-(S)-6-amino-4,5,6,7-tetrahydrobenzo[d]thiazole were designed, synthesized and evaluated for their anti-leukemic activity by trypan blue exclusion, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH) assays and cell cycle analysis. Results suggest that the position, number and bulkiness of the substituent on the phenyl ring of aryl carboxamide moiety at 2nd position of 6-amino-4,5,6,7-tetrhydrobenzo[d]thiazole play a key role in inhibiting the proliferation of leukemia cells. Compounds with ortho substitution showed poor activity and with meta and para substitution showed good activity.


Assuntos
Leucemia/patologia , Tiazóis/síntese química , Tiazóis/farmacologia , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas por Ionização por Electrospray , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , Tiazóis/química
4.
Invest New Drugs ; 28(4): 454-65, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19506804

RESUMO

Benzothiazoles are multitarget agents with broad spectrum of biological activity. Among the antitumor agents discovered in recent years, the identification of various 2-(4-aminophenyl) benzothiazoles as potent and selective antitumor drugs against different cancer cell lines has stimulated remarkable interest. Some of the benzothiazoles are known to induce cell cycle arrest, activation of caspases and interaction with DNA molecule. Based on these interesting properties of benzothiazoles and to obtain new biologically active agents, a series of novel 4,5,6,7-tetrahydrobenzo[d]thiazole derivatives 5(a-i) were synthesized and evaluated for their efficacy as antileukemic agents in human leukemia cells (K562 and Reh). The chemical structures of the synthesized compounds were confirmed by (1)H NMR, LCMS and IR analysis. The cytotoxicity of these compounds were determined using trypan blue exclusion, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. Results showed that, these compounds mediate a significant cytotoxic response to cancer cell lines tested. We found that the compounds having electron withdrawing groups at different positions of the phenyl ring of the thiourea moiety displayed significant cytotoxic effect with IC(50) value less than 60 microM. To rationalize the role of electron withdrawing group in the induction of cytotoxicity, we have chosen molecule 5g (IC(50) approximately 15 microM) which is having chloro substitution at ortho and para positions. Flow cytometric analysis of annexin V-FITC/ propidium iodide (PI) double staining and DNA fragmentation suggest that 5g can induce apoptosis.


Assuntos
Benzotiazóis/síntese química , Benzotiazóis/farmacologia , Leucemia/tratamento farmacológico , Apoptose/efeitos dos fármacos , Benzotiazóis/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Fragmentação do DNA/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Células K562 , Estrutura Molecular , Relação Estrutura-Atividade
5.
Arch Pharm Res ; 32(10): 1335-43, 2009 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-19898794

RESUMO

The present work deals with the anticancer effect of benzimidazole derivatives associated with the pyridine framework. By varying the functional group at N-terminal of the benzimidazole by different L-amino acids, several 2-(4-(2,2,2-trifluoroethoxy)-3-methylpyridin-2-ylthio)-1Hbenzo[d]imidazole derivatives 9(a-j) were synthesized. Their chemical structures were confirmed by (1)H NMR, IR and mass spectroscopic techniques. The synthesized compounds were examined for their antiproliferative effects against human leukemia cell lines, K562 and CEM. The preliminary results showed most of the derivatives had moderate antitumor activity. Compound 9j containing cysteine residue exhibited good inhibition compared to other amino acid resides. In addition DNA fragmentation results suggest that 9j is more cytotoxic and able to induce apoptosis.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Benzimidazóis/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Fragmentação do DNA/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
6.
Bioorg Med Chem ; 16(9): 5157-63, 2008 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-18359231

RESUMO

A series of novel, potent, and selective muscarinic receptor 1 agonists (M1 receptor agonists) that employ a key N-substituted morpholine Arecoline moiety has been synthesized as part of research effort for the therapy of Alzheimer's diseases. The ester group of arecoline (which is reported as muscarinic agonist) has been replaced by N-substituted morpholine ring. The structure-activity relationship reveals that the electron donating 4-substituted sulfonyl derivatives (9a, 9b, 9c, and 9e) on the nitrogen atom of the morpholine ring increases the affinity of M1 receptor binding 50- to 80-fold greater than the corresponding arecoline. Other derivatives also showed considerable M1 receptor binding affinity.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Modelos Animais de Doenças , Morfolinas/farmacologia , Morfolinas/uso terapêutico , Receptor Muscarínico M1/agonistas , Sulfonamidas/química , Doença de Alzheimer/induzido quimicamente , Animais , Ligação Competitiva , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Memória/efeitos dos fármacos , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Estrutura Molecular , Morfolinas/química , Ratos , Ratos Wistar , Escopolamina , Estereoisomerismo , Relação Estrutura-Atividade
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