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1.
Eur J Med Chem ; 194: 112245, 2020 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-32220687

RESUMO

Antibacterial-resistance speaks to an overall alarm, particularly in regards to the flare-up of methicillin-resistance Staphylococcus aureus (MRSA), a classic reason for genuine skin and flimsy tissues diseases. Clinically noteworthy antibacterial-resistance is probably the best challenge of the 21st century. Notwithstanding, new-fangled antibiotics are right now being created at a much more slow pace than our developing requirement for such drugs. The intriguing atomic structure of indole ring makes them appropriate possibility for the drug advancement. In this scaled down survey we abridge novel indole-based derivatives potency against diverse bacterial strains. Specifically, we plot the connection between the different structures of altered indole derivatives along with its antibacterial movement against multidrug-resistance MRSA could be discussed. This prepared information may fill in as a target for the adjustment of accessible molecules to plan new powerful antibacterial agents with lesser side effects.


Assuntos
Antibacterianos/farmacologia , Indóis/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Antibacterianos/química , Relação Dose-Resposta a Droga , Farmacorresistência Bacteriana/efeitos dos fármacos , Indóis/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
2.
Eur J Med Chem ; 173: 117-153, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-30995567

RESUMO

At present more than 250 FDA approved chlorine containing drugs were available in the market and many pharmaceutically important drug candidates in pre-clinical trials. Thus, it is quite obvious to expect that in coming decades there will be an even greater number of new chlorine-containing pharmaceuticals in market. Chlorinated compounds represent the family of compounds promising for use in medicinal chemistry. This review describes the recent advances in the synthesis of chlorine containing heterocyclic compounds as diverse biological agents and drugs in the pharmaceutical industries for the inspiration of the discovery and development of more potent and effective chlorinated drugs against numerous death-causing diseases.


Assuntos
Antibacterianos/farmacologia , Antimaláricos/farmacologia , Antineoplásicos/farmacologia , Descoberta de Drogas , Inibidores de Glicosídeo Hidrolases/farmacologia , Hidrocarbonetos Clorados/farmacologia , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antimaláricos/síntese química , Antimaláricos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Hidrocarbonetos Clorados/síntese química , Hidrocarbonetos Clorados/química , Estrutura Molecular
3.
Bioorg Chem ; 76: 113-129, 2018 02.
Artigo em Inglês | MEDLINE | ID: mdl-29169078

RESUMO

Amino acids/peptide conjugated heterocycles represent an important class of therapeutical agents. Biologically active heterocycles are conjugated with amino acids or peptides to increase the drug resistance. Furthermore, the amino acid/peptide based drugs have low toxicity, ample bioavailability and permeability, modest potency and good metabolic and pharmacokinetic properties. Synthetic amino acid/peptides based heterocyclic conjugates constitute a promising choice for the development of new, less toxic and safer conventional pharmaceutical drugs in the near future. In this review, we discuss and highlight the recent findings of the structural features that encourage biological applications of amino acid/peptides based conjugates.


Assuntos
Aminoácidos/farmacologia , Peptídeos/farmacologia , Aminoácidos/química , Animais , Anti-Infecciosos/química , Antineoplásicos/química , Humanos , Peptídeos/química
4.
Anticancer Agents Med Chem ; 18(4): 488-505, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29110622

RESUMO

Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.


Assuntos
Antineoplásicos/farmacologia , Descoberta de Drogas , Neoplasias/tratamento farmacológico , Sulfonamidas/farmacologia , Compostos de Sulfonilureia/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias/patologia , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química , Compostos de Sulfonilureia/síntese química , Compostos de Sulfonilureia/química
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