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1.
Mol Divers ; 23(3): 723-738, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30560342

RESUMO

A series of new urea/thiourea derivatives 3a-j were synthesized by simple addition reaction of functionalized phenyl isocyanates/isothiocyanates 2a-j with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine (imatinib intermediate) (1) in the presence of 1,4-dimethyl piperazine (DMPZ) as a base, and another series of new sulfonamide/carbamate derivatives 5a-k were synthesized by reacting 1 with various substituted aromatic sulfonyl chlorides 4a-f and aromatic/aliphatic chloroformates 4g-k in the presence of DMPZ as a base. The title compounds 3a-j and 5a-k were characterized by IR, 1H, 13C NMR and mass spectral data. Antimicrobial, antioxidant and in silico molecular docking studies were made against aromatase.


Assuntos
Carbamatos/química , Mesilato de Imatinib/síntese química , Mesilato de Imatinib/farmacologia , Simulação de Acoplamento Molecular , Sulfonamidas/química , Tioureia/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Aromatase/química , Aromatase/metabolismo , Técnicas de Química Sintética , Mesilato de Imatinib/química , Mesilato de Imatinib/metabolismo , Conformação Proteica , Análise Espectral , Relação Estrutura-Atividade
2.
Antiviral Res ; 95(2): 118-27, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22659095

RESUMO

A series of novel substituted dihydropyrimidine and 5H-thiazolo [3, 2-a] pyrimidine derivatives were designed and synthesized as a potential target to discover drugs fighting against the viral diseases. The main objective of the present work is to carry out the QSAR studies for all the series of the compounds starting from 4a to 6j to find out their molecular descriptors and predict the biological properties. All of them are showing the best QSAR descriptors, hence chosen for the prediction of anti-viral activity against Newcastle disease virus (NDV). Initially their inhibitory activity was predicted by molecular docking of these compounds against haemaglutinin-neuraminidase (HN) protein using molecular operating environment (MOE) software. Based on the best affinity and highest docking scores 4b, 5b and 6b were assayed in vivo on NDV infected chicks and it was found that there is significant improvement in the survival of the chicks with the treatment (P<0.05). 4b and 6b showed better curative effect than 5b at the dose concentration of 40 mg/kg body weight of chicks. The results from molecular docking study and biological assays can be inferred to consider these molecules as potential antiviral drugs.


Assuntos
Antivirais/química , Antivirais/farmacologia , Vírus da Doença de Newcastle/efeitos dos fármacos , Pirimidinas/química , Pirimidinas/farmacologia , Animais , Antivirais/administração & dosagem , Galinhas , Simulação de Dinâmica Molecular , Doença de Newcastle/tratamento farmacológico , Doenças das Aves Domésticas/tratamento farmacológico , Pirimidinas/administração & dosagem , Relação Quantitativa Estrutura-Atividade , Análise de Sobrevida
3.
Chem Pharm Bull (Tokyo) ; 51(7): 860-3, 2003 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-12843597

RESUMO

N-(substituted)-N'-(2,3-dihydro-5-benzoyl-2-oxido-1H-1,3,2-benzodiazaphosphol-2-yl) ureas were synthesized by reacting 3,4-diaminobenzophenone (4) with different chlorides of carbamidophosphoric acids (3) in the presence of triethylamine at 40-45 degrees C. Their 1H-, 13C- and 31P-NMR spectral data are discussed. The title compounds were screened for antifungal and antibacterial activity against the fungi Aspergillus niger and Fusarium solani and bacteria Escherichia coli and Staphylococcus aureus. These compounds showed higher antibacterial activity when compared with antifungal activity.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana/métodos , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento
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