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1.
Eur J Med Chem ; 157: 1081-1095, 2018 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-30179746

RESUMO

Methicillin-resistant Staphylococcus aureus (MRSA) is the most common pathogen both in hospital and community settings, and is capable of causing serious and even fatal infections. Several antibiotics have been approved for the treatment of infections caused by MRSA, but MRSA has already developed resistance to them. More than ever, it's imperative to develop novel, high effective and fast acting anti-MRSA agents. Quinolones are one of the most common antibiotics in clinical practice used to treat various bacterial infections, and some of them displayed excellent in vitro and in vivo anti-MRSA activities, so quinolone derivatives are one of the most promising candidates. This review summarizes the recent developments of quinolone derivatives with potential activity against MRSA, and the structure-activity relationship is also discussed.


Assuntos
Antibacterianos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Quinolonas/química , Quinolonas/farmacologia , Infecções Estafilocócicas/tratamento farmacológico , Animais , Antibacterianos/química , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
2.
Curr Top Med Chem ; 18(2): 101-113, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29473509

RESUMO

Bis-coumarins have caused great interests in the recent years. These compounds exhibit diverse biological activities which are ascribed to their ability to exert noncovalent interactions with the various active sites in organisms. Some of them such as dicoumarolum and dicoumarol were approved for therapeutic purposes in clinical practice. Encouraged by the above facts, numerous biscoumarin derivatives have been synthesized and screened for their biological activities, and many of them showed promising potency. This review is focused on the biological potential of bis-coumarin derivatives with particular mention of those exhibiting antibacterial, anticoagulant, antiinflammatory, antiviral, anti-parasite and antitumor activities, and their structure-activity relationships are also discussed.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Anticoagulantes/farmacologia , Antineoplásicos/farmacologia , Antiparasitários/farmacologia , Cumarínicos/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Anticoagulantes/síntese química , Anticoagulantes/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antiparasitários/síntese química , Antiparasitários/química , Cumarínicos/síntese química , Cumarínicos/química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
3.
Eur J Med Chem ; 139: 429-440, 2017 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-28818767

RESUMO

One-third of the world's population infected tuberculosis (TB), and more than 1 million deaths annually. The co-infection between the mainly pathogen Mycobacterium tuberculosis (MTB) and HIV, and the incidence of drug-resistant TB, multi-drug resistant TB, extensively drug-resistant TB as well as totally drug-resistant TB have further aggravated the mortality and spread of this disease. Thus, there is an urgent need to develop novel anti-TB agents against both drug-susceptible and drug-resistant TB. The wide spectrum of biological activities and successful utilization of pyrazole-containing drugs in clinic have inspired more and more attention towards this kind of heterocycles. Numerous of pyrazole-containing derivatives have been synthesized for searching new anti-TB agents, and some of them showed promising potency and may have novel mechanism of action. This review aims to outline the recent achievements in pyrazole-containing derivatives as anti-TB agents and their structure-activity relationship.


Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Pirazóis/farmacologia , Tuberculose/tratamento farmacológico , Antituberculosos/síntese química , Antituberculosos/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Pirazóis/síntese química , Pirazóis/química , Relação Estrutura-Atividade
4.
Eur J Med Chem ; 138: 501-513, 2017 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-28692915

RESUMO

Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, threats one-third of the world's population. Although numerous efforts have been undertaken to develop new anti-TB agents, only a handful of compounds have entered human trials in the past 5 decades. Triazoles including 1,2,3-triazole and 1,2,4-triazole are one of the most important classes of nitrogen containing heterocycles that exhibited various biological activities. Triazole derivatives are regarded as a new class of effective anti-TB candidates owing to their potential anti-TB potency. Thus, molecules containing triazole moiety may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistant to certain extent. This review outlines the advances in the application of triazole-containing hybrids as anti-TB agents, and discusses the structure-activity relationship of these derivatives.


Assuntos
Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Triazóis/farmacologia , Tuberculose/tratamento farmacológico , Antituberculosos/química , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/química
5.
Ying Yong Sheng Tai Xue Bao ; 21(3): 668-74, 2010 Mar.
Artigo em Zh | MEDLINE | ID: mdl-20560323

RESUMO

Taking three flue-cured tobacco (Nicotiana tabacum L.) varieties Y5, Y7, and NC89 as test objects, this paper studied the effects of nitrogen fertilization on their leaf senescence, photosynthetic characteristics, yield, and quality. Increasing nitrogen supply increased the leaf superoxide dismutase (SOD) activity, chlorophyll content, and photosynthetic performance, and decreased the leaf malondialdehyde (MDA) content significantly. Accordingly, the leaf senescence was delayed. Compared with Y5 and NC89, variety Y7 had higher leaf MDA content and lower leaf SOD activity, chlorophyll content, and photosynthetic performance, and thus, its leaves senesced faster. High quality tobacco leaves with higher average price, gross value, superior leaves percentage, and reasonable chemical constituents were harvested under the application of 45 kg N x hm(-2), compared with applying 60 and 75 kg N x hm(-2). It was suggested that different flue-cured tobacco varieties had obvious differences in their leaf senescence physiological characteristics, and nitrogen fertilization played important roles in regulating their leaf senescence, yield, and quality. Appropriate nitrogen fertilization could improve the quality of tobacco leaves, and achieve higher economic benefits.


Assuntos
Biomassa , Nicotiana/crescimento & desenvolvimento , Nitrogênio/farmacologia , Fotossíntese , Folhas de Planta/fisiologia , Fertilizantes , Folhas de Planta/crescimento & desenvolvimento , Controle de Qualidade , Superóxido Dismutase/metabolismo , Nicotiana/genética
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