0000000000896807

AUTHOR

Ralph Holl

showing 3 related works from this author

Bioactive pyrrole-based compounds with target selectivity

2020

The discovery of novel synthetic compounds with drug-like properties is an ongoing challenge in medicinal chemistry. Natural products have inspired the synthesis of compounds for pharmaceutical application, most of which are based on N-heterocyclic motifs. Among these, the pyrrole ring is one of the most explored heterocycles in drug discovery programs for several therapeutic areas, confirmed by the high number of pyrrole-based drugs reaching the market. In the present review, we focused on pyrrole and its hetero-fused derivatives with anticancer, antimicrobial, and antiviral activities, reported in the literature between 2015 and 2019, for which a specific target was identified, being resp…

Coronavirus disease 2019 (COVID-19)Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)Antineoplastic AgentsReview ArticlePyrroleAntiviral Agentschemistry.chemical_compoundAnti-Infective AgentsDrug DiscoveryHumansPyrrolesMolecular Targeted TherapyAntiviralTargeted compoundsPyrrolePharmacologyDrug discoveryChemistryOrganic ChemistryCOVID-19Biological activityGeneral MedicineAntimicrobialSettore CHIM/08 - Chimica FarmaceuticaCombinatorial chemistryAnticancerDrug DesignAntimicrobialPharmacophoreSelectivityEuropean Journal of Medicinal Chemistry
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Pyrrolidine in Drug Discovery: A Versatile Scaffold for Novel Biologically Active Compounds

2021

AbstractThe five-membered pyrrolidine ring is one of the nitrogen heterocycles used widely by medicinal chemists to obtain compounds for the treatment of human diseases. The great interest in this saturated scaffold is enhanced by (1) the possibility to efficiently explore the pharmacophore space due to sp3-hybridization, (2) the contribution to the stereochemistry of the molecule, (3) and the increased three-dimensional (3D) coverage due to the non-planarity of the ring—a phenomenon called “pseudorotation”. In this review, we report bioactive molecules with target selectivity characterized by the pyrrolidine ring and its derivatives, including pyrrolizines, pyrrolidine-2-one, pyrrolidine-2…

Steric effectsPyrrolidinesMolecular StructureChemistryDrug discoveryEnantioselective synthesisStereoisomerismGeneral ChemistryReviewAnti-inflammatory and analgesic agentsRing (chemistry)Combinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticaPyrrolidineProlinolPyrrolidinechemistry.chemical_compoundAntidiabeticsDrug DiscoveryPseudorotationHumansAnticancer and antibacterial agentsPharmacophoreCentral nervous system diseases
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Editorial: Emerging heterocycles as bioactive compounds

2023

Heterocycles represent a privileged scaffold due to their ability to interact with biological systems via heteroatoms. It is no coincidence that every year the Food and Drug Administration approves numerous new drugs that contain at least one heterocyclic system as active pharmacophoric part in their structure. Many heterocyclic compounds with therapeutic properties, including anticancer, antimicrobial, anti-inflammatory and so on, come from natural sources such as plants and animals, and medicinal chemists very often use them to study their chemical space and improve their biological activity. In fact, several efficient approaches for the formation of aromatic heterocyclic compounds and th…

heterocycles new chemical entities natural products purine nucleoside phosphorylase pantetheinase sulfhydrylase activity quinazolineGeneral ChemistrySettore CHIM/08 - Chimica FarmaceuticaFrontiers in Chemistry
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