Indole, a fundamental heterocyclic core, has emerged as a cornerstone in the medicinal chemistry due to its diverse biological activities and structural versatility. This aromatic compound, present in natural as well as synthetic compounds, offers a versatile platform for the drug discovery. By strategically incorporating functional groups or pharmacophores, researchers can tailor indole-derivatives to target a wide range of diseases. This review delves into the multifaceted applications of indole derivatives, highlighting their potential as therapeutic agents for cancer, diabetes, depression, Alzheimer's diseases, Parkinson's disease, etc. emphasizing how indole derivatives can enhance potency and selectivity. By understanding the structure-activity relationship of indole compounds, scientists can develop innovative drug candidates with improved therapeutic profiles. The review highlights the diverse nature of indole-based derivatives along with the structure-activity relationshipThe current review comprehensively covers the advancements and developments in the field over the past seven years, specifically from 2017 to 2024. This timeframe was selected to provide an up-to-date and thorough analysis of recent progress, capturing significant trends, breakthroughs, and emerging insights within the domain. By focusing on this period, the review ensures relevance and highlights the evolving landscape of research, offering a detailed synthesis of key findings and their implications for future studies.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bioorg.2024.108092 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The Complex Relationship Between Cannabis Use and Mental Health: Considering the Influence of Cannabis Use Patterns and Individual Factors.
CNS Drugs
January 2025
Cognitive and Clinical Neuroimaging Core, McLean Hospital, McLean Imaging Center, Belmont, MA, USA.
The relationship between cannabis use and mental health is complex, as studies often report seemingly contradictory findings regarding whether cannabis use results in more positive or negative treatment outcomes. With an increasing number of individuals using cannabis for both recreational (i.e.
View Article and Find Full Text PDFHigh-density multielectrode arrays bring cellular resolution to neuronal activity and network analyses of corticospinal motor neurons.
Sci Rep
January 2025
Department of Neurology, Feinberg School of Medicine, Northwestern University, 303 E. Chicago Ave, Chicago, IL, 60611, USA.
Corticospinal motor neurons (CSMN), located in the motor cortex of the brain, are one of the key components of the motor neuron circuitry. They are in part responsible for the initiation and modulation of voluntary movement, and their degeneration is the hallmark for numerous diseases, such as amyotrophic lateral sclerosis (ALS), hereditary spastic paraplegia, and primary lateral sclerosis. Cortical hyperexcitation followed by in-excitability suggests the early involvement of cortical dysfunction in ALS pathology.
View Article and Find Full Text PDFDiscovery of potent anti-toxoplasmosis drugs from secondary metabolites in Citrus limon (lemon) leaves, supported in-silico study.
Sci Rep
January 2025
Department of Zoonotic Diseases, National Research Centre, Dokki, Giza, 12622, Egypt.
Toxoplasmosis induced by Toxoplasma gondii is a well-known health threat, that prompts fatal encephalitis increased with immunocompromised patients, in addition, it can cause chorioretinitis, microcephaly, stillbirth in the fetus and even led to death. Standard therapy uses sulfadiazine and pyrimethamine drugs revealed beneficial results during the acute stage, however, it has severe side effects. UPLC-ESI-MS/MS used to explore C.
View Article and Find Full Text PDFA membrane permeability database for nonpeptidic macrocycles.
Sci Data
January 2025
Department of Chemistry-BMC, Uppsala University, SE-75123, Uppsala, Sweden.
The process of developing new drugs is arduous and costly, particularly for targets classified as "difficult-to-drug." Macrocycles show a particular ability to modulate difficult-to-drug targets, including protein-protein interactions, while still allowing oral administration. However, the determination of membrane permeability, critical for reaching intracellular targets and for oral bioavailability, is laborious and expensive.
View Article and Find Full Text PDFEvaluation of Machine Learning/Molecular Mechanics End-State Corrections with Mechanical Embedding to Calculate Relative Protein-Ligand Binding Free Energies.
J Chem Theory Comput
January 2025
Exscientia, Schrödinger Building, Oxford Science Park, Oxford OX4 4GE, U.K.
The development of machine-learning (ML) potentials offers significant accuracy improvements compared to molecular mechanics (MM) because of the inclusion of quantum-mechanical effects in molecular interactions. However, ML simulations are several times more computationally demanding than MM simulations, so there is a trade-off between speed and accuracy. One possible compromise are hybrid machine learning/molecular mechanics (ML/MM) approaches with mechanical embedding that treat the intramolecular interactions of the ligand at the ML level and the protein-ligand interactions at the MM level.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!