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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
Mini Rev Med Chem ; 21(10): 1152-1172, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33319670


Quinoline derivatives are considered broad-spectrum pharmacological compounds that exhibit a wide range of biological activities. Integration of quinoline moiety can improve its physical and chemical properties and also pharmacological behavior. Due to its wide range of pharmaceutical applications, it is a very popular compound to design new drugs for the treatment of multiple diseases like cancer, dengue fever, malaria, tuberculosis, fungal infections, AIDS, Alzheimer's disease and diabetes. In this review, our major focus is to pay attention to the biological activities of quinoline compounds in the treatment of these diseases such as anti-viral, anti-cancer, anti-malarial, antibacterial, anti-fungal, anti-tubercular and anti-diabetic.

Neoplasias/tratamento farmacológico , Quinolinas/farmacologia , Síndrome de Imunodeficiência Adquirida/tratamento farmacológico , Doença de Alzheimer/tratamento farmacológico , Dengue/tratamento farmacológico , Diabetes Mellitus/tratamento farmacológico , Humanos , Malária/tratamento farmacológico , Micoses/tratamento farmacológico , Quinolinas/síntese química , Quinolinas/química , Tuberculose/tratamento farmacológico
J Heterocycl Chem ; 2020 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-33362294


A one-pot quick and efficient multicomponent reaction has been developed for the synthesis of a new series of functionalized 8-hydroxy-4-phenyl-1,2-dihydroquinoline derivatives using 30 mol% ammonium acetate in ethanol as solvent. This economical protocol run smoothly to give variety of quinoline derivatives in 55% to 98% yield from inexpensive reagents and catalyst in mild reaction conditions. Various spectroscopic techniques like FTIR, 1H NMR and 13C NMR, MALDI-TOF-MS, and EI-MS were used to study and confirm their structure.

Heliyon ; 6(9): e05035, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33020745


We have developed a new and facile one pot three component protocol catalyzed by ammonium acetate for construction of new functionalized 7-hydroxy-4-phenyl-1,2-dihydroquinoline derivatives. A variety of quinoline derivatives were obtained in good to excellent yield from inexpensive reagents and catalyst in mild reaction conditions that provide atom economy and cost efficacy. Various spectroscopic techniques like FTIR, 1HNMR and 13CNMR were employed to study their structure while mass of the synthesized compounds were confirmed through MALDI-TOF-MS and EI mass spectrometry.

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