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1.
Environ Sci Pollut Res Int ; 30(43): 97965-97976, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37603239

RESUMO

Due to the pressing need to combat climate change, reaching carbon neutrality-defined as having net-zero greenhouse gas emissions-has elevated to the status of a worldwide priority. While non-financial policies concentrate on regulation and incentives to promote environmentally friendly behavior, green financial policies strive to move investment toward low-carbon and sustainable initiatives. Therefore, the study aims to examine how green financial and non-financial policies affect carbon neutrality in China from 1995 to 2021. For analyzing the linear and nonlinear estimates, the study has employed the autoregressive distributed lag (ARDL) and nonlinear autoregressive distributed lag (NARDL) frameworks. The findings suggest that in the linear framework, green finance policies and environmental policy stringency encourage renewable energy consumption and discourage CO2 emissions. In the nonlinear framework, the positive shocks in the green finance policies and environmental policy stringency increase renewable energy consumption, and the negative shock in both types of policies discourages renewable energy consumption. In the CO2 model, a positive shock in green finance policies and environmental policy stringency reduces CO2 emissions, and a negative change in both these policies is insignificant. Since the positive and negative changes in both these policies significantly and differently impact renewable energy consumption and CO2 emissions; thus, policymakers should take into account positive and negative changes in both these policies while formulating policies for carbon neutrality targets in China.


Assuntos
Dióxido de Carbono , Política Fiscal , Condições Sociais , Políticas , Carbono
2.
J Med Chem ; 63(17): 9623-9649, 2020 09 10.
Artigo em Inglês | MEDLINE | ID: mdl-32787097

RESUMO

The rise of multidrug resistant (MDR) Gram-negative (GN) pathogens and the decline of available antibiotics that can effectively treat these severe infections are a major threat to modern medicine. Developing novel antibiotics against MDR GN pathogens is particularly difficult as compounds have to permeate the GN double membrane, which has very different physicochemical properties, and have to circumvent a plethora of resistance mechanisms such as multiple efflux pumps and target modifications. The bacterial type II topoisomerases DNA gyrase (GyrA2B2) and Topoisomerase IV (ParC2E2) are highly conserved targets across all bacterial species and validated in the clinic by the fluoroquinolones. Dual inhibitors targeting the ATPase domains (GyrB/ParE) of type II topoisomerases can overcome target-based fluoroquinolone resistance. However, few ATPase inhibitors are active against GN pathogens. In this study, we demonstrated a successful strategy to convert a 2-carboxamide substituted azaindole chemical scaffold with only Gram-positive (GP) activity into a novel series with also potent activity against a range of MDR GN pathogens. By systematically fine-tuning the many physicochemical properties, we identified lead compounds such as 17r with a balanced profile showing potent GN activity, high aqueous solubility, and desirable PK features. Moreover, we showed the bactericidal efficacy of 17r using a neutropenic mouse thigh infection model.


Assuntos
Carbolinas/química , Carbolinas/farmacologia , DNA Girase/metabolismo , DNA Topoisomerase IV/metabolismo , Desenho de Fármacos , Escherichia coli/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Trifosfato de Adenosina/metabolismo , Animais , DNA Girase/química , DNA Topoisomerase IV/química , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Escherichia coli/enzimologia , Camundongos , Modelos Moleculares , Conformação Proteica , Staphylococcus aureus/enzimologia
3.
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
4.
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
5.
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
6.
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
7.
Ying Yong Sheng Tai Xue Bao ; 21(3): 668-74, 2010 Mar.
Artigo em Chinês | 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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