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Molecules ; 26(16)2021 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-34443460


Synthetic heterocyclic compounds have incredible potential against different diseases; pyridines, phenolic compounds and the derivatives of azo moiety have shown excellent antimicrobial, antiviral, antidiabetic, anti-melanogenic, anti-ulcer, anticancer, anti-mycobacterial, anti-inflammatory, DNA binding and chemosensing activities. In the present review, the above-mentioned activities of the nitrogen-containing heterocyclic compounds (pyridines), hydroxyl (phenols) and azo derivatives are discussed with reference to the minimum inhibitory concentration and structure-activity relationship, which clearly indicate that the presence of nitrogen in the phenyl ring; in addition, the hydroxyl substituent and the incorporation of a diazo group is crucial for the improved efficacies of the compounds in probing different diseases. The comparison was made with the reported drugs and new synthetic derivatives that showed recent therapeutic perspectives made in the last five years.

Compostos Azo/uso terapêutico , Fenóis/uso terapêutico , Piridinas/uso terapêutico , Compostos Azo/síntese química , Compostos Azo/química , Imageamento Tridimensional , Fenóis/síntese química , Fenóis/química , Piridinas/síntese química , Piridinas/química
J Enzyme Inhib Med Chem ; 36(1): 1509-1520, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34238110


In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-resistant strain and P. vulgaris (gram-negative). The IC50 (µg/mL) of TR-1 was found to be most effective (15.70 ± 1.3 µg/mL) compared to the reference drug acarbose (21.59 ± 1.5 µg/mL), hence, it was further selected for the kinetic studies in order to illustrate the mechanism of inhibition. The enzyme inhibitory kinetics and mode of binding for the most active inhibitor (TR-1) was performed which showed that the compound is a non-competitive inhibitor and effectively inhibits the target enzyme by binding to its binuclear active site reversibly.

Antibacterianos/farmacologia , Compostos Azo/farmacologia , Inibidores Enzimáticos/farmacologia , Hipoglicemiantes/farmacologia , Simulação de Acoplamento Molecular , alfa-Glucosidases/metabolismo , Antibacterianos/síntese química , Antibacterianos/química , Compostos Azo/síntese química , Compostos Azo/química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Escherichia coli/efeitos dos fármacos , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Cinética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Saccharomyces cerevisiae/enzimologia , Staphylococcus aureus/efeitos dos fármacos
Cell Mol Biol (Noisy-le-grand) ; 66(7): 169-173, 2020 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-33287937


Colorectal cancer is a life-threatening and therapeutically challenging disease. Increasingly it is being deciphered that genetic and epigenetic mutations play a central role in cancer onset and progression. Excitingly, discovery of non-coding RNAs is considered to be a milestone in molecular oncology and emerging evidence is deepening our understanding about pivotal role of miRNAs in carcinogenesis. miR-143 has been experimentally verified to play an instrumental role as tumor suppressor. Recent studies suggest that single nucleotide polymorphisms rs41291957 and rs353292 in miR-143 may associate with the progression and or development of colorectal cancer. In present study 400 Pakistani subjects participated including 200 colorectal cancer patients and 200 age and gender matched healthy individuals. Blood samples and clinical information of the confirmed patients was collected from cancer diagnosis and treatment hospitals in Pakistan. The polymorphisms rs41291957 and rs353292 were genotyped in patients and controls by Polymerase Chain Reaction-Restriction Fragment Length Polymorphism (PCR-RFLP) and results were validated by Sanger sequencing. The association of the SNPs within the study group was analyzed by χ² test with p value < 0.05 as significant. Odds ratio was calculated with 95% confidence interval.Genetic predisposition to cancer was observed in presence of characteristic rs45291957 polymorphism. χ² test results show strongly significant association mi-RNA rs45291957 SNP with colorectal cancer p value 0.0111 (<0.05) along with the statistically significant correlation tested by odds ratio with 95% confidence interval. However, no significant correlation (p value 0.6683) could be found for the association of rs353292 with colorectal cancer in Pakistani population. The present study for the first time gave evidence of miR-143 rs41291957 involvement in colorectal cancer patients of Pakistani population. This target can be a useful molecular tool for the prognosis and treatment targets for colorectal cancer in Pakistani population. rs353292 genetic association can be explored for different cancers in Pakistan to completely rule out its role in cancer.

Cureus ; 11(9): e5791, 2019 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-31728238


Objective To determine the relationship between physical activity and depression between the two genders amongst the young adults of Islamabad. Methods We conducted a cross-sectional study of students who were studying in various colleges and universities of Islamabad. Students who were willing to participate in the study and who were studying in the institute for more than six months were included in the study. The data was collected through a self-reporting questionnaire and a self-constructed questionnaire. Cronbach's alpha was used to assess the internal consistency of the self-constructed questionnaire, and it was found to be 0.69. The data obtained were analyzed on IBM's Statistical Package for the Social Sciences (SPSS) version 21 (IBM, Armonk, NY, US). Results Out of 298 participants, 113 (38%) were males and 185 (62%) were females. The mean age of the participants was 21.60±1.39 years. One-hundred twenty-six participants were found most likely to suffer from depression. Out of these 126 participants, 42 (33%) were females and 84 (67%) were males. Thirty-nine percent of the participants reported fatigue and inability to attend to their normal routine. Pearson correlation was calculated for the association of depression and age, and it was found to be significant (p-value less than 0.05). The correlation for depression with respect to physical activity was also found to be significant (p-value less than 0.05). Conclusions Low levels of physical activity can be a major risk factor for the development of depression and the possible exacerbation of any pre-existing mental disorder. There is a need to combat this problem to decrease the use of pharmaceutical means for curing depression.

Mini Rev Med Chem ; 19(9): 708-719, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30058483


In this review, specific therapeutic and medicinal advantages including antiviral, antibacterial, antifungal and antitumor, strategies for drug designing, structure-activity relationship, advances in the syntheses of azo and hippuric acid derivatives of more than 50 compounds have been discussed since 2009-2018. It is found that phenyl-diazenyl azo derivatives and pyridinyl substituted hippuric acid derivatives showed promising antiretroviral potential. The incorporation of azo functionality to the respective quinolones and coumarin moieties and the insertion of thiocarbazone to hippuric acid displayed immense antibacterial activities. While, azo and hippuric acid derivatives of triazole and phenyl species gave maximum fungicidal as well as cytotoxic activities.

Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Compostos Azo/química , Compostos Azo/farmacologia , Hipuratos/química , Hipuratos/farmacologia , Animais , Anti-Infecciosos/síntese química , Antineoplásicos/síntese química , Compostos Azo/síntese química , Infecções Bacterianas/tratamento farmacológico , Desenho de Fármacos , Hipuratos/síntese química , Humanos , Micoses/tratamento farmacológico , Neoplasias/tratamento farmacológico , Relação Estrutura-Atividade , Viroses/tratamento farmacológico