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1.
Curr Top Med Chem ; 2024 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-39069705

RESUMO

Phyllanthus emblica, popularly mentioned as amla or Indian gooseberry, has attracted a lot of interest lately because of its varied phytochemical makeup and related pharmacological properties. The phytochemistry, historical applications, bioactive makeup, and pharmacological properties of Phyllanthus emblica fruits are all summarised in this paper. This review emphasises the rich phytochemical profile of Phyllanthus emblica, which contains flavonoids, tannins, alkaloids, and polyphenolic chemicals, through a thorough assessment of the literature. Furthermore, the historical value of Phyllanthus emblica as a therapeutic agent for a variety of health issues is shown by its traditional applications in numerous indigenous medical systems. The bioactive makeup of Phyllanthus emblica fruits, especially its high polyphenol and vitamin C content, is responsible for its hepatoprotective, antioxidant, and anti-inflammatory qualities. Moreover, new pharmacological research has clarified its potential for the cure of neurological illnesses, tumor, diabetes, and cardiovascular diseases. In order to shed light on the pharmacological properties of Phyllanthus emblica fruits and suggest future avenues for study, this review compiles the body of scientific data that is already accessible. All things considered, Phyllanthus Emblica shows great promise as a natural resource with significant applications in complementary and alternative medicine and pharmacological research.

2.
Med Chem ; 2024 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-38920062

RESUMO

One important class of organic compounds having many uses, especially in medical chemistry, is benzothiophene and its derivatives. This review examines the biological activity of benzothiophene derivatives and summarizes the synthetic methods used in their production. The effectiveness of several synthetic pathways, such as cyclization techniques, functional group modifications, and reactions catalyzed by transition metals, in gaining access to benzothiophene scaffolds has been examined. Additionally, a broad spectrum of therapeutic domains, such as antiinflammatory, antibacterial, antidiabetic, anticancer, antimicrobial, anti-leishmanial, antifungal, antimalarial, and antitubercular activities, are covered by the pharmacological activities that are being explored. The synthesis and pharmacological potential of benzothiophene derivatives are well-explained in this thorough review, which opens up new options for medicinal chemistry and drug discovery study. Overall, this study is a useful resource for scientists working on drug development and discovery as it sheds light on the pharmacological potential of benzothiophene derivatives. This review includes the synthesis and bioactivities of the years 2002-2024. The goal of this review is to compile the existing information on benzothiophene derivatives and provide guidance for future research and development as well as insights into their possible medicinal uses.

3.
Curr Top Med Chem ; 24(17): 1504-1528, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38818908

RESUMO

Benzimidazole is a privileged drug design and discovery scaffold with various pharmacological activities, including antimicrobial, anticancer, antitubercular, anti-inflammatory, antidiabetic, antihypertensive, antimalarial, and many more. This scaffold can be observed in the structure of numerous FDA-approved drugs and employed in medicinal chemistry to develop novel bioactive compounds through rational drug design. Its broad pharmacological significance is due to physicochemical attributes, including H-bond donor-acceptor efficiency, π-π stacking interactions, and hydrophobic interactions; these characteristics enable benzimidazole derivatives to bind with macromolecules efficiently. This article emphasizes mechanisms, SAR, and docking studies to unveil benzimidazole's various active hybrids accountable for diversified activities. It will assist researchers in strategically designing various novel benzimidazole-endowed hybrids to develop clinically active therapeutic candidates.


Assuntos
Benzimidazóis , Desenho de Fármacos , Descoberta de Drogas , Benzimidazóis/química , Benzimidazóis/farmacologia , Benzimidazóis/síntese química , Humanos , Relação Estrutura-Atividade , Estrutura Molecular , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/síntese química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/síntese química
4.
Comb Chem High Throughput Screen ; 27(14): 2043-2061, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38243956

RESUMO

Neurodegeneration causes premature death in the peripheral and central nervous system. Neurodegeneration leads to the accumulation of oxidative stress, inflammatory responses, and the generation of free radicals responsible for nervous disorders like amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, and Huntington's disorders. Therefore, focus must be diverted towards treating and managing these disorders, as it is very challenging. Furthermore, effective therapies are also lacking, so the growing interest of the global market must be inclined towards developing newer therapeutic approaches that can intercept the progression of neurodegeneration. Emerging evidences of research findings suggest that antioxidant therapy has significant potential in modulating disease phenotypes. This makes them promising candidates for further investigation. This review focuses on the role of oxidative stress and reactive oxygen species in the pathological mechanisms of various neurodegenerative diseases, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, and Huntington's disorders and their neuroprotection. Additionally, it highlights the potential of antioxidant-based therapeutics in mitigating disease severity in humans and improving patient compliance. Ongoing extensive global research further sheds light on exploring new therapeutic targets for a deeper understanding of disease mechanisms in the field of medicine and biology targeting neurogenerative disorders.


Assuntos
Antioxidantes , Doenças Neurodegenerativas , Estresse Oxidativo , Humanos , Estresse Oxidativo/efeitos dos fármacos , Doenças Neurodegenerativas/tratamento farmacológico , Doenças Neurodegenerativas/metabolismo , Antioxidantes/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Animais , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química
5.
Med Chem ; 20(4): 385-396, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38173200

RESUMO

Quinoline-5,8-diones, also referred to as 5,8-quinolinediones or quinolinequinones, have been researched extensively for their antiproliferative effects, where they displayed great results. Other than anticancer, they exhibit multiple activities such as antimalarial, antiviral, antibacterial, and antifungal activities. Natural quinolinequinones have also been known for their significant activities. The review highlights the diverse biological activities exhibited by synthetic quinoline- 5,8-diones over the past two decades. Continued research in this field is warranted to fully exploit the therapeutic potential of these intriguing compounds and their derivatives for future drug development. By comprehensively evaluating the therapeutic applications and biological activities of quinoline-5,8-dione derivatives, this review endeavors to provide researchers and practitioners with a valuable resource that will foster informed decision-making and inspire further investigations into harnessing the immense potential of this intriguing scaffold for the benefit of human health.


Assuntos
Quinolinas , Humanos , Quinolinas/química , Quinolinas/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/química , Animais , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Antifúngicos/farmacologia , Antifúngicos/química , Antifúngicos/síntese química , Estrutura Molecular , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/síntese química
6.
Med Chem ; 20(2): 115-129, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-37855281

RESUMO

Chromenes are a significant family of heterocyclic chemicals that have a wide range of biological applications, a simple chemical structure, and only mildly undesirable side effects. The synthesis of a wide range of chromene analogs that displayed unexpected behaviors via numerous mechanisms was investigated by a number of different research teams, which led to the discovery of multiple pathways for their synthesis. In addition, different chromene-fused heterocycles exhibit a wide variety of fascinating biological actions, including those that are anticancer, anticonvulsant, antibacterial, anticholinesterase, antituberculosis, and anti-diabetic. In light of this, the purpose of this study is to highlight the many synthesis techniques and antibacterial activity associated with chromene-fused heterocyclic compounds. Moreover, such research can open avenues for exploring other therapeutic applications of these compounds in various disease areas, as their biological activities extend beyond antibacterial effects.


Assuntos
Anti-Infecciosos , Compostos Heterocíclicos , Compostos Heterocíclicos/farmacologia , Compostos Heterocíclicos/química , Benzopiranos/farmacologia , Benzopiranos/química , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Anticonvulsivantes
7.
Fitoterapia ; 172: 105764, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38042505

RESUMO

A member of the Valerianacae family, Nardostachys jatamansi is the smallest, most primitive, perennial, dwarf, hairy, rhizomatous, herbaceous species. It has an enlarged antiquity of usage as ayurvedic medicine, homeopathic medicine, ethnomedicine, and the Indian system of medicine, and is now used in the modern medicine industry. In the ayurvedic medical system, the rhizomes of the plant are used as a bitter tonic, stimulant, antispasmodic, epileptic treatment, and for hysteria. Pharmacological reports on Nardostachys jatamansi revealed its antifungal activity, hepatoprotective activity, central nervous system activity, anticonvulsant activity, neuroprotective activity, antiparkinson's activity, antioxidant activity, antidiabetic activity, tranquilizing activity, antiestrogenic activity furthermore, Jatamansone has also been linked to anti-hypertensive, anti-arrhythmic, anti-asthmatic, nematicidal, and antibacterial effects. This review article's objective is to go over traditional uses, Phytochemistry, Ethnomedicinal Importance, pharmacological activities, precise procedures for variety improvement, protection, and appropriate utilization, and recognize prospects for Nardostachys jatamansi.


Assuntos
Nardostachys , Estrutura Molecular , Medicina Tradicional , Rizoma , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
8.
Chem Biol Drug Des ; 102(4): 921-938, 2023 10.
Artigo em Inglês | MEDLINE | ID: mdl-37232059

RESUMO

Diabetes mellitus (DM) is a serious global health concern affecting over 500 million people. To put it simply, it is one of the most dangerous metabolic illnesses. Insulin resistance is the root cause of 90% of all instances of diabetes, all of which are classified as Type 2 DM. Untreated, it poses a hazard to civilization since it can lead to terrifying consequences and even death. Oral hypoglycemic medicines presently available act in a variety of ways, targeting various organs and pathways. The use of protein tyrosine phosphatase 1B (PTP1B) inhibitors, on the contrary, is a novel and effective method of controlling type 2 diabetes. PTP1B is a negative insulin signaling pathway regulator; hence, inhibiting PTP1B increases insulin sensitivity, glucose absorption, and energy expenditure. PTP1B inhibitors also restore leptin signaling and are considered a potential obesity target. In this review, we have compiled a summary of the most recent advances in synthetic PTP1B inhibitors from 2015 to 2022 which have scope to be developed as clinical antidiabetic drugs.


Assuntos
Diabetes Mellitus Tipo 2 , Resistência à Insulina , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Insulina , Obesidade/tratamento farmacológico , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo
9.
Chem Biol Drug Des ; 102(3): 587-605, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37070386

RESUMO

Twenty different infectious disorders induced by bacteria, viruses, and parasites are categorized as neglected tropical diseases (NTDs) by WHO. The severity of chagas disease remains a major concern in endemic areas and an emerging public health hazard in nonendemic countries. Trypanosoma cruzi, the etiological agent of this NTD, is mostly transmitted by triatomine vectors and comprises a range of epidemiologically significant variants. Current chemotherapeutics are obsolete, and one of the primary reasons for treatment cessation is their poor safety and effectiveness. Due to the aforementioned challenges, researchers are now focusing on discovering alternative novel safe, and economically reachable therapies for the treatment of trypanosomiasis. Certain target-based drugs that target specific biochemical processes of the causative parasites have been described as potential antichagasic agents that possesses various types of heterocyclic scaffolds. These flexible molecules have a wide range of biological actions, and various synthesized compounds with strong activity have been documented. This review aims to discuss the available literature on synthetic anti-T. cruzi drugs that will give a food for thought to medicinal chemists thriving to design and develop such drugs. Furthermore, some of the studies discussed herein are concerned with the potential of novel drugs to block new viable sites in T. cruzi.


Assuntos
Doença de Chagas , Tripanossomicidas , Trypanosoma cruzi , Humanos , Tripanossomicidas/farmacologia , Tripanossomicidas/uso terapêutico , Tripanossomicidas/química , Doença de Chagas/tratamento farmacológico , Sistemas de Liberação de Medicamentos
10.
Curr Neurovasc Res ; 20(1): 162-169, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36733199

RESUMO

Apolipoprotein E4 (APOE4) is one of the primary genetic risk factors for late-onset of Alzheimer's disease (AD). While its primary function is to transport cholesterol, it also regulates metabolism, aggregation, and deposition of amyloid-ß (Aß) in the brain. The disruption in the generation and removal of Aß in the brain is the primary cause of memory and cognitive loss and thus plays a significant role in the development of AD. In several prior genetic investigations, the APOE4 allele has been linked to higher susceptibility to severe acute respiratory syndrome (SARSCoV- 2) infection and COVID-19 mortality. However, information on the involvement of APOE4 in the underlying pathology and clinical symptoms is limited. Due to the high infection and mortality rate of COVID-19 in AD individuals, challenges have been identified in the management of AD patients during the COVID-19 pandemic. In order to provide evidence-based, more effective healthcare, it is critical to identify underlying concerns and, preferably, biomarkers. The risk variant APOE4 imparts enhanced infectivity by the underlying coronavirus SARS-CoV-2 at a cellular level, genetic level, and route level. Here we review existing advances in clinical and basic research on the AD-related gene APOE, as well as the role of APOE in AD pathogenesis, using neurobiological evidence. Moreover, the role of APOE in severe COVID-19 in Alzheimer's patients has also been reviewed.


Assuntos
Doença de Alzheimer , Apolipoproteína E4 , COVID-19 , Humanos , Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/metabolismo , Apolipoproteína E4/genética , Apolipoproteína E4/metabolismo , Encéfalo/metabolismo , COVID-19/metabolismo , Pandemias , SARS-CoV-2
11.
Comb Chem High Throughput Screen ; 25(11): 1838-1858, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34809541

RESUMO

The entire world has been in a battle against the COVID-19 pandemic since its first appearance in December 2019. Thus researchers are desperately working to find an effective and safe therapeutic agent for its treatment. The multifunctional coronavirus enzyme papain-like protease (PLpro) is a potential target for drug discovery to combat the ongoing pandemic responsible for cleavage of the polypeptide, deISGylation, and suppression of host immune response. The present review collates the in silico studies performed on various FDA-approved drugs, chemical compounds, and phytochemicals from various drug databases and represents the compounds possessing the potential to inhibit PLpro. Thus this review can provide quick access to a potential candidate to medicinal chemists to perform in vitro and in vivo experiments who are thriving to find the effective agents for the treatment of COVID-19.


Assuntos
Tratamento Farmacológico da COVID-19 , Antivirais/química , Antivirais/farmacologia , Antivirais/uso terapêutico , Humanos , Pandemias , Papaína/química , Peptídeo Hidrolases , Compostos Fitoquímicos , Inibidores de Proteases/farmacologia , Inibidores de Proteases/uso terapêutico
12.
Curr Pharm Biotechnol ; 22(12): 1591-1601, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33504302

RESUMO

Coronavirus-19 is a severe acute respiratory disorder in humans which has become a major health problem. It spreads out very rapidly throughout the world since it has been first identified in Wuhan, China (December 2019). The causative virus is known as severe acute respiratory syndrome coronavirus 2. And the World Health Organization has named this respiratory syndrome as a new epidemic disease called COVID-19. The incidence of COVID-19 continued to increase with three million confirmed infected cases and with 244,000 death cases worldwide. Until now there is no specific treatment or vaccine available against COVID- 19. The collective information about the different aspects of COVID-19 viral infection has been gathered from renowned journals, and electronic databases including Science Direct, Web of Science, Scopus and PubMed from 1990 to 2020. This manuscript has highlighted the transmission and symptoms of Covid-19. Therefore, these studies show how the SARS-CoV 2 can facilitate the debut of the virus into targeted host cells.


Assuntos
COVID-19 , China/epidemiologia , Surtos de Doenças , Humanos , SARS-CoV-2
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