Designing Next-Generation Drug-Like Molecules for Medicinal Applications

The development of new drugs/drug candidates for medical treatment remains an exciting but challenging process as only a limited number of synthetic compounds fit well into the discovery and development process after multiple experimentation and screening efforts in search of their preclinical prope...

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प्रकाशित: MDPI - Multidisciplinary Digital Publishing Institute 2025
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ऑनलाइन पहुंच:ONIX_20250220_9783725830084_520
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collection Directory of Open Access Books
description The development of new drugs/drug candidates for medical treatment remains an exciting but challenging process as only a limited number of synthetic compounds fit well into the discovery and development process after multiple experimentation and screening efforts in search of their preclinical properties. Over the years, this continuous demand has been fueled by the use of organic/synthetic chemistry protocols that deliver new molecules or improve the existing toolbox diversifying libraries of pharmacophores of medicinal interest. The application of new methodologies particularly employing green and sustainable commercial feedstock chemicals for the discovery and development of biological therapeutics opens up new avenues of research. In parallel, the discovery and development of new organic molecules have always proved effective in designing drugs while overcoming critical challenges to the pharmaceutical industry and providing innovative solutions toward commercialized medicines. This reprint aims to provide a far-reaching overview of the most recent developments in synthetic methodologies as well as medicinal chemistry applications of small-molecule inhibitors.
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publisherStr MDPI - Multidisciplinary Digital Publishing Institute
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spelling doab-20.500.12854ir-1531562025-02-20T13:38:59Z Designing Next-Generation Drug-Like Molecules for Medicinal Applications Khan, Imtiaz Zaib, Sumera anthraquinones antidiabetic antimicrobial Cassia obtusifolia L. hepatoprotection neuro protection spirooxindole azomethine ylides [3+2] cycloaddition reaction anti-cancer activity amide anti-inflammatory COX-2 iNOS NO PGE2 pyrazole quinoline thiosemicarbazone molecular design hybridization Alzheimer’s disease neurodegeneration drug therapy cholinesterases enzyme inhibition molecular docking diabetes drug delivery α-glucosidase in vivo studies α-mangostin nanosponges quasi-emulsion method HER4 ErbB4 cancer kinase inhibitors structure-activity relationship hesperetin derivatives PTP1B hesperetin 5-O-glucoside baricitinib bioavailability encapsulation hybrid nanoparticles poly(d,l-lactide-coglycolide) stearin anticancer kinase inhibitor neurodegenerative disorders deep machine learning generative modeling kinase inhibitor design Bruton’s tyrosine kinase covalent inhibitors 3-phenyl-β-alanine 1,3,4-oxadiazole hybrids carbonic anhydrase-II dental caries biofilm glucosyltransferases virtual screening antibiofilm antimicrobial ADMET profiling triterpenoic acid ursolic acid oleanolic acid betulinic acid rhodamine B rhodamine 101 cytotoxicity SARS-CoV-2 nsp16-nsp10 2′-o-methyltransferase FDA approved drugs molecular fingerprints structural similarity MD simulations MMPBSA immunomodulatory apoptosis in silico studies nicotinamide VEGFR-2 amino acyl coumarins (pseudo)-dipeptidyl coumarins carbonic anhydrases (CAs) monoamine oxidases (MAOs) iodinated histidines membrane active peptides anticryptococcal activity iodopeptides pore formation cell lysis antifungal agents n/a 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 The development of new drugs/drug candidates for medical treatment remains an exciting but challenging process as only a limited number of synthetic compounds fit well into the discovery and development process after multiple experimentation and screening efforts in search of their preclinical properties. Over the years, this continuous demand has been fueled by the use of organic/synthetic chemistry protocols that deliver new molecules or improve the existing toolbox diversifying libraries of pharmacophores of medicinal interest. The application of new methodologies particularly employing green and sustainable commercial feedstock chemicals for the discovery and development of biological therapeutics opens up new avenues of research. In parallel, the discovery and development of new organic molecules have always proved effective in designing drugs while overcoming critical challenges to the pharmaceutical industry and providing innovative solutions toward commercialized medicines. This reprint aims to provide a far-reaching overview of the most recent developments in synthetic methodologies as well as medicinal chemistry applications of small-molecule inhibitors. 2025-02-20T13:38:57Z 2025-02-20T13:38:57Z 2025 book ONIX_20250220_9783725830084_520 9783725830084 9783725830077 https://directory.doabooks.org/handle/20.500.12854/153156 eng application/octet-stream Attribution 4.0 International https://mdpi.com/books/pdfview/book/10429 MDPI - Multidisciplinary Digital Publishing Institute 10.3390/books978-3-7258-3007-7 10.3390/books978-3-7258-3007-7 46cabcaa-dd94-4bfe-87b4-55023c1b36d0 9783725830084 9783725830077 398 Basel open access
spellingShingle anthraquinones
antidiabetic
antimicrobial
Cassia obtusifolia L.
hepatoprotection
neuro protection
spirooxindole
azomethine ylides
[3+2] cycloaddition reaction
anti-cancer activity
amide
anti-inflammatory
COX-2
iNOS
NO
PGE2
pyrazole
quinoline
thiosemicarbazone
molecular design
hybridization
Alzheimer’s disease
neurodegeneration
drug therapy
cholinesterases
enzyme inhibition
molecular docking
diabetes
drug delivery
α-glucosidase
in vivo studies
α-mangostin
nanosponges
quasi-emulsion method
HER4
ErbB4
cancer
kinase inhibitors
structure-activity relationship
hesperetin derivatives
PTP1B
hesperetin 5-O-glucoside
baricitinib
bioavailability
encapsulation
hybrid nanoparticles
poly(d,l-lactide-coglycolide)
stearin
anticancer
kinase inhibitor
neurodegenerative disorders
deep machine learning
generative modeling
kinase inhibitor design
Bruton’s tyrosine kinase
covalent inhibitors
3-phenyl-β-alanine 1,3,4-oxadiazole hybrids
carbonic anhydrase-II
dental caries
biofilm
glucosyltransferases
virtual screening
antibiofilm
antimicrobial ADMET profiling
triterpenoic acid
ursolic acid
oleanolic acid
betulinic acid
rhodamine B
rhodamine 101
cytotoxicity
SARS-CoV-2 nsp16-nsp10 2′-o-methyltransferase
FDA approved drugs
molecular fingerprints
structural similarity
MD simulations
MMPBSA
immunomodulatory
apoptosis
in silico studies
nicotinamide
VEGFR-2
amino acyl coumarins
(pseudo)-dipeptidyl coumarins
carbonic anhydrases (CAs)
monoamine oxidases (MAOs)
iodinated histidines
membrane active peptides
anticryptococcal activity
iodopeptides
pore formation
cell lysis
antifungal agents
n/a
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
Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title_full Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title_fullStr Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title_full_unstemmed Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title_short Designing Next-Generation Drug-Like Molecules for Medicinal Applications
title_sort designing next generation drug like molecules for medicinal applications
topic anthraquinones
antidiabetic
antimicrobial
Cassia obtusifolia L.
hepatoprotection
neuro protection
spirooxindole
azomethine ylides
[3+2] cycloaddition reaction
anti-cancer activity
amide
anti-inflammatory
COX-2
iNOS
NO
PGE2
pyrazole
quinoline
thiosemicarbazone
molecular design
hybridization
Alzheimer’s disease
neurodegeneration
drug therapy
cholinesterases
enzyme inhibition
molecular docking
diabetes
drug delivery
α-glucosidase
in vivo studies
α-mangostin
nanosponges
quasi-emulsion method
HER4
ErbB4
cancer
kinase inhibitors
structure-activity relationship
hesperetin derivatives
PTP1B
hesperetin 5-O-glucoside
baricitinib
bioavailability
encapsulation
hybrid nanoparticles
poly(d,l-lactide-coglycolide)
stearin
anticancer
kinase inhibitor
neurodegenerative disorders
deep machine learning
generative modeling
kinase inhibitor design
Bruton’s tyrosine kinase
covalent inhibitors
3-phenyl-β-alanine 1,3,4-oxadiazole hybrids
carbonic anhydrase-II
dental caries
biofilm
glucosyltransferases
virtual screening
antibiofilm
antimicrobial ADMET profiling
triterpenoic acid
ursolic acid
oleanolic acid
betulinic acid
rhodamine B
rhodamine 101
cytotoxicity
SARS-CoV-2 nsp16-nsp10 2′-o-methyltransferase
FDA approved drugs
molecular fingerprints
structural similarity
MD simulations
MMPBSA
immunomodulatory
apoptosis
in silico studies
nicotinamide
VEGFR-2
amino acyl coumarins
(pseudo)-dipeptidyl coumarins
carbonic anhydrases (CAs)
monoamine oxidases (MAOs)
iodinated histidines
membrane active peptides
anticryptococcal activity
iodopeptides
pore formation
cell lysis
antifungal agents
n/a
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 anthraquinones
antidiabetic
antimicrobial
Cassia obtusifolia L.
hepatoprotection
neuro protection
spirooxindole
azomethine ylides
[3+2] cycloaddition reaction
anti-cancer activity
amide
anti-inflammatory
COX-2
iNOS
NO
PGE2
pyrazole
quinoline
thiosemicarbazone
molecular design
hybridization
Alzheimer’s disease
neurodegeneration
drug therapy
cholinesterases
enzyme inhibition
molecular docking
diabetes
drug delivery
α-glucosidase
in vivo studies
α-mangostin
nanosponges
quasi-emulsion method
HER4
ErbB4
cancer
kinase inhibitors
structure-activity relationship
hesperetin derivatives
PTP1B
hesperetin 5-O-glucoside
baricitinib
bioavailability
encapsulation
hybrid nanoparticles
poly(d,l-lactide-coglycolide)
stearin
anticancer
kinase inhibitor
neurodegenerative disorders
deep machine learning
generative modeling
kinase inhibitor design
Bruton’s tyrosine kinase
covalent inhibitors
3-phenyl-β-alanine 1,3,4-oxadiazole hybrids
carbonic anhydrase-II
dental caries
biofilm
glucosyltransferases
virtual screening
antibiofilm
antimicrobial ADMET profiling
triterpenoic acid
ursolic acid
oleanolic acid
betulinic acid
rhodamine B
rhodamine 101
cytotoxicity
SARS-CoV-2 nsp16-nsp10 2′-o-methyltransferase
FDA approved drugs
molecular fingerprints
structural similarity
MD simulations
MMPBSA
immunomodulatory
apoptosis
in silico studies
nicotinamide
VEGFR-2
amino acyl coumarins
(pseudo)-dipeptidyl coumarins
carbonic anhydrases (CAs)
monoamine oxidases (MAOs)
iodinated histidines
membrane active peptides
anticryptococcal activity
iodopeptides
pore formation
cell lysis
antifungal agents
n/a
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_9783725830084_520