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1.
J Genet Eng Biotechnol ; 15(2): 331-334, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30647671

RESUMO

Microbial lipases owing to their broad substrate specificity are widely used in various industrial applications like food processing, organic synthesis, detergent formulation and oil manufacturing. In the current study the immobilized lipase from Lactobacillus plantarum was found novel in degrading meat which can be applied in medical field and also in synthesizing different short chain fatty acid esters like 2,3,4-hydroxybenzyl acetates and triazole ester which makes a great impingement in natural flavor industry. The 4-hydroxybenzyl acetate obtained can also be used in cosmetics.

2.
Org Biomol Chem ; 14(3): 876-83, 2016 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-26592542

RESUMO

The synthesis and anti-cancer activity evaluation of fused imidazoquinoline compounds is reported in this paper. Yb(OTf)3 has been utilized as a catalyst for the synthesis of 1,4-diaryl substituted imidazo[4,5-c]quinolines via a modified Pictet-Spengler approach. The desired imidazole ring was synthesized from imines using TosMIC (toluenesulfonylmethyl isocyanide) and subsequently functionalized at the C-4 position yielding an imidazoquinoline skeleton. Importantly, the final step was carried out without the aid of any prefunctionalization to obtain the resultant compounds in good yields. The synthesized compounds, when screened for anti-cancer activity, revealed the highest activity with 4-(2-bromophenyl)-1-phenyl-1H-imidazo[4,5-c]quinoline (IC50: 103.3 µM).


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Imidazóis/farmacologia , Quinolinas/farmacologia , Animais , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Imidazóis/síntese química , Imidazóis/química , Camundongos , Estrutura Molecular , Quinolinas/síntese química , Quinolinas/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas
3.
Chempluschem ; 81(12): 1339-1348, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31964065

RESUMO

The bipyridine-based constructs 4-(pyridine-2-yl)-3H-pyrrolo[2,3-c]quinoline (PPQ) and [6-(3H-pyrrolo[2,3-c]quinolin-4-yl)pyridin-2-yl]methanol (PPQ-OH) and their assemblies with surfactants are evaluated as turn-on fluorescent sensors for Zn2+ ions in aqueous solution. This study strives to overcome the problem of low water solubility of the hydrophobic PPQ and PPQ-OH by using micelles. Whereas the ligands show selective sensing behavior for Zn2+ over important biological cations including Na+ , K+ , Ca2+ , Mg2+ in anionic sodium dodecyl sulfate and non-ionic Tween 80 micelles, no Zn2+ sensing is observed in cationic cetyltrimethylammonium bromide micelles. Unlike in DMF, Cd2+ interference is observed in aqueous conditions, which can be avoided either by performing the study at pH≥9 or by carrying out a time-resolved fluorescence study. Analysis of the Job plot data, the fluorescence lifetimes, and experiments on varying micellar shape and pH, confirms that the coordination volume of the resulting octahedral metal complex and formation of a five-membered chelate ring are critical factors for Cd2+ interference. The described sensing systems are capable of detecting Zn2+ ions at the micromolar level. Additionally, it is shown that PPQ and PPQ-OH can be used to detect Zn2+ in HeLa cells under physiological conditions in bioimaging studies.

4.
Org Biomol Chem ; 13(9): 2600-5, 2015 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-25574832

RESUMO

A facile synthesis of 4-aryl substituted oxazolo[4,5-c]quinolines has been described via a modified Pictet-Spengler method and using Cu(TFA)2 as a catalyst. The developed methodology directly functionalizes the C-4 position of oxazoles without the aid of any prefunctionalization, in the presence of the more reactive C-2 position in good yields. The versatility of the established method has been demonstrated by its application in the synthesis of 4-substituted oxazolo-[1,8]naphthyridine ring systems.


Assuntos
Oxazóis/química , Quinolinas/síntese química , Estrutura Molecular , Quinolinas/química
5.
J Arthroplasty ; 26(1): 1-8, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20056374

RESUMO

An independent single surgeon's 7-year experience with Birmingham hip resurfacing is presented. The study also involved investigation of the significance of pedestal sign in patients requiring revision. A consecutive 117 hips in 101 patients (59 male and 42 female patients) operated on by the senior author (VGJ) were assessed at a mean follow-up of 7 years (range, 5-9.4 years). Mean age at surgery was 54 years (range, 20-74 years). Seventy-three hips had a preoperative diagnosis of primary osteoarthritis, and secondary osteoarthritis was seen in 44 hips. Failure was defined as revision for any reason. Revision of the femoral component alone was undertaken in 8 hips (6.8%): 5 within first year for periprosthetic fracture neck of femur and in 3 hips after 5 years of follow-up. In 2 patients who were known to have osteonecrosis of the femoral head preoperatively, the femoral component progressively collapsed into varus after 5 years of follow-up. Pedestal sign was the earliest radiologic sign noted in these 2 patients and progressed rapidly within 1 year on serial radiographs well before the onset of clinical symptoms. Kaplan-Meier survival with revision as end point at 7 years was 91.5% (95% confidence interval, 97.6%-85.4%).


Assuntos
Artroplastia de Quadril/instrumentação , Prótese de Quadril/classificação , Prótese de Quadril/normas , Osteoartrite do Quadril/cirurgia , Adulto , Idoso , Feminino , Fraturas do Colo Femoral/diagnóstico por imagem , Fraturas do Colo Femoral/cirurgia , Necrose da Cabeça do Fêmur/diagnóstico por imagem , Necrose da Cabeça do Fêmur/cirurgia , Seguimentos , Humanos , Estimativa de Kaplan-Meier , Estudos Longitudinais , Masculino , Pessoa de Meia-Idade , Fraturas Periprotéticas/diagnóstico por imagem , Fraturas Periprotéticas/cirurgia , Radiografia , Reoperação
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