Heterocyclic Compounds in Medicinal Chemistry

Although current medicinal chemistry landscapes seem to have changed thanks to the great advent of modern biological drugs, small molecules remain of crucial prominance in the identification of new drugs. Indeed, small molecules exert therapeutically favorable advantages, such as oral administration...

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collection Directory of Open Access Books
description Although current medicinal chemistry landscapes seem to have changed thanks to the great advent of modern biological drugs, small molecules remain of crucial prominance in the identification of new drugs. Indeed, small molecules exert therapeutically favorable advantages, such as oral administration, tailored distribution, cell membrane crossing, accessible synthesis, and standardization. As a result, heterocycle-based small-molecule drugs represent the majority fraction of drugs currently marketed or in development. On the other side, the pharmacokinetic and pharmacodynamic properties, such as potency, selectivity, lipophilicity, polarity and water solubility can be modulated through the strategic inclusion of heterocycles in the molecule. Furthermore, heterocycles provide a fertile ground for the optimization of drug candidates due to their adaptable ability to hydrogen bond with target proteins, and the high prevalence of rings containing oxygen, sulfur, and nitrogen derives from their widespread presence in a wide range of natural products, whose structural motifs have always been emulated by the efforts of medicinal chemistry. Taking all these aspects into account, this Special Issue has collected new studies and new perspectives on the topic, further emphasizing the challenges that are still open and possible in the field of medicinal chemistry.
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spelling doab-20.500.12854ir-1528402025-02-20T13:09:26Z Heterocyclic Compounds in Medicinal Chemistry Madia, Valentina Noemi Ialongo, Davide cyclin-dependent kinase kinase inhibitor COVID-19 229E coronavirus pyrrole synthesis DFT antioxidant SH-SY5Y cellular toxicity cell protection benzo[b]furans benzofurans anticancer antibacterial antifungal medicinal chemistry drug discovery 4-aminocoumarin Schiff bases urease inhibition molecular docking antibacterial activity MD simulation indole hydrazone MCF7 apoptosis kinase inhibition pyrimidines building block antibiotic antiviral immunological treatment neurological disorders anti-inflammatory chronic pain diabetes mellitus benzofuran hybrid structure NSCLC EGFR Annona squamosa L. endophytic fungi MRSA ADME prediction public health molecular docking-coupled dynamics simulation lipophilicity diquinothiazines ADME chromatography phenothiazines anticancer agents 1H-benzo[d]imidazole tyrosine kinase inhibitor multiple kinase inhibitor cancer JBJ-125 deep learning pharmacophore virtual screening molecular dynamics ADMET 3,5-disubstituted hydantoins preparative HPLC separation NMR analysis absolute configuration CD/VCD antiproliferative activity in silico biological profiling thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general thema EDItEUR::P Mathematics and Science::PH Physics::PHH Thermodynamics and heat Although current medicinal chemistry landscapes seem to have changed thanks to the great advent of modern biological drugs, small molecules remain of crucial prominance in the identification of new drugs. Indeed, small molecules exert therapeutically favorable advantages, such as oral administration, tailored distribution, cell membrane crossing, accessible synthesis, and standardization. As a result, heterocycle-based small-molecule drugs represent the majority fraction of drugs currently marketed or in development. On the other side, the pharmacokinetic and pharmacodynamic properties, such as potency, selectivity, lipophilicity, polarity and water solubility can be modulated through the strategic inclusion of heterocycles in the molecule. Furthermore, heterocycles provide a fertile ground for the optimization of drug candidates due to their adaptable ability to hydrogen bond with target proteins, and the high prevalence of rings containing oxygen, sulfur, and nitrogen derives from their widespread presence in a wide range of natural products, whose structural motifs have always been emulated by the efforts of medicinal chemistry. Taking all these aspects into account, this Special Issue has collected new studies and new perspectives on the topic, further emphasizing the challenges that are still open and possible in the field of medicinal chemistry. 2025-02-20T13:09:24Z 2025-02-20T13:09:24Z 2024 book ONIX_20250220_9783725822928_204 9783725822928 9783725822911 https://directory.doabooks.org/handle/20.500.12854/152840 eng application/octet-stream Attribution 4.0 International https://mdpi.com/books/pdfview/book/10045 MDPI - Multidisciplinary Digital Publishing Institute 10.3390/books978-3-7258-2291-1 10.3390/books978-3-7258-2291-1 46cabcaa-dd94-4bfe-87b4-55023c1b36d0 9783725822928 9783725822911 384 Basel open access
spellingShingle cyclin-dependent kinase
kinase inhibitor
COVID-19
229E
coronavirus
pyrrole
synthesis
DFT
antioxidant
SH-SY5Y
cellular toxicity
cell protection
benzo[b]furans
benzofurans
anticancer
antibacterial
antifungal
medicinal chemistry
drug discovery
4-aminocoumarin
Schiff bases
urease inhibition
molecular docking
antibacterial activity
MD simulation
indole
hydrazone
MCF7
apoptosis
kinase inhibition
pyrimidines
building block
antibiotic
antiviral
immunological treatment
neurological disorders
anti-inflammatory
chronic pain
diabetes mellitus
benzofuran
hybrid structure
NSCLC
EGFR
Annona squamosa L.
endophytic fungi
MRSA
ADME prediction
public health
molecular docking-coupled dynamics simulation
lipophilicity
diquinothiazines
ADME
chromatography
phenothiazines
anticancer agents
1H-benzo[d]imidazole
tyrosine kinase inhibitor
multiple kinase inhibitor
cancer
JBJ-125
deep learning
pharmacophore
virtual screening
molecular dynamics
ADMET
3,5-disubstituted hydantoins
preparative HPLC separation
NMR analysis
absolute configuration
CD/VCD
antiproliferative activity
in silico biological profiling
thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general
thema EDItEUR::P Mathematics and Science::PH Physics::PHH Thermodynamics and heat
Heterocyclic Compounds in Medicinal Chemistry
title Heterocyclic Compounds in Medicinal Chemistry
title_full Heterocyclic Compounds in Medicinal Chemistry
title_fullStr Heterocyclic Compounds in Medicinal Chemistry
title_full_unstemmed Heterocyclic Compounds in Medicinal Chemistry
title_short Heterocyclic Compounds in Medicinal Chemistry
title_sort heterocyclic compounds in medicinal chemistry
topic cyclin-dependent kinase
kinase inhibitor
COVID-19
229E
coronavirus
pyrrole
synthesis
DFT
antioxidant
SH-SY5Y
cellular toxicity
cell protection
benzo[b]furans
benzofurans
anticancer
antibacterial
antifungal
medicinal chemistry
drug discovery
4-aminocoumarin
Schiff bases
urease inhibition
molecular docking
antibacterial activity
MD simulation
indole
hydrazone
MCF7
apoptosis
kinase inhibition
pyrimidines
building block
antibiotic
antiviral
immunological treatment
neurological disorders
anti-inflammatory
chronic pain
diabetes mellitus
benzofuran
hybrid structure
NSCLC
EGFR
Annona squamosa L.
endophytic fungi
MRSA
ADME prediction
public health
molecular docking-coupled dynamics simulation
lipophilicity
diquinothiazines
ADME
chromatography
phenothiazines
anticancer agents
1H-benzo[d]imidazole
tyrosine kinase inhibitor
multiple kinase inhibitor
cancer
JBJ-125
deep learning
pharmacophore
virtual screening
molecular dynamics
ADMET
3,5-disubstituted hydantoins
preparative HPLC separation
NMR analysis
absolute configuration
CD/VCD
antiproliferative activity
in silico biological profiling
thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general
thema EDItEUR::P Mathematics and Science::PH Physics::PHH Thermodynamics and heat
topic_facet cyclin-dependent kinase
kinase inhibitor
COVID-19
229E
coronavirus
pyrrole
synthesis
DFT
antioxidant
SH-SY5Y
cellular toxicity
cell protection
benzo[b]furans
benzofurans
anticancer
antibacterial
antifungal
medicinal chemistry
drug discovery
4-aminocoumarin
Schiff bases
urease inhibition
molecular docking
antibacterial activity
MD simulation
indole
hydrazone
MCF7
apoptosis
kinase inhibition
pyrimidines
building block
antibiotic
antiviral
immunological treatment
neurological disorders
anti-inflammatory
chronic pain
diabetes mellitus
benzofuran
hybrid structure
NSCLC
EGFR
Annona squamosa L.
endophytic fungi
MRSA
ADME prediction
public health
molecular docking-coupled dynamics simulation
lipophilicity
diquinothiazines
ADME
chromatography
phenothiazines
anticancer agents
1H-benzo[d]imidazole
tyrosine kinase inhibitor
multiple kinase inhibitor
cancer
JBJ-125
deep learning
pharmacophore
virtual screening
molecular dynamics
ADMET
3,5-disubstituted hydantoins
preparative HPLC separation
NMR analysis
absolute configuration
CD/VCD
antiproliferative activity
in silico biological profiling
thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general
thema EDItEUR::P Mathematics and Science::PH Physics::PHH Thermodynamics and heat
url ONIX_20250220_9783725822928_204