Structural modification aimed for improving solubility of lead compounds in early phase drug discovery
Many lead compounds fail to reach clinical trials despite being potent because of low
bioavailability attributed to their insufficient solubility making solubility a primary and crucial …
bioavailability attributed to their insufficient solubility making solubility a primary and crucial …
Recent advances in the chemistry of pyrazoles. Properties, biological activities, and syntheses
A Schmidt, A Dreger - Current Organic Chemistry, 2011 - benthamdirect.com
Pyrazoles are of considerable interest due to the broad variety of their biological activities.
This overview summarizes structures of pharmacologically interesting pyrazoles, natural …
This overview summarizes structures of pharmacologically interesting pyrazoles, natural …
Drug-like property concepts in pharmaceutical design
L Di, EH Kerns, GT Carter - Current pharmaceutical design, 2009 - ingentaconnect.com
The pharmaceutical industry is facing an ever increasing challenge to deliver safer and
more effective medicines. Traditionally, drug discovery programs were driven solely by …
more effective medicines. Traditionally, drug discovery programs were driven solely by …
Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements
A Hall, M Chatzopoulou, J Frost - Bioorganic & Medicinal Chemistry, 2024 - Elsevier
Carboxylic acids are key pharmacophoric elements in many molecules. They can be seen
as a problem by some, due to perceived permeability challenges, potential for high plasma …
as a problem by some, due to perceived permeability challenges, potential for high plasma …
Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells
XL Ding, HY Zhang, L Qi, BX Zhao, S Lian… - Bioorganic & medicinal …, 2009 - Elsevier
A series of novel 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxamide derivatives 3a–l, were
synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with …
synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with …
Efficient parallel synthesis of privileged benzopyranylpyrazoles via regioselective condensation of β-keto aldehydes with hydrazines
In this study, the practical construction of a pilot library with benzopyranylpyrazole, a novel
core skeleton synthesized through the recombination of privileged structures, benzopyran …
core skeleton synthesized through the recombination of privileged structures, benzopyran …
ADME profiling in drug discovery and development: an overview
T Bohnert, C Prakash - Encyclopedia of drug metabolism and …, 2011 - Wiley Online Library
The applications of parallel synthesis and combinatory chemistry to expedite lead finding
and lead optimization processes have shifted the chemical libraries toward poorer …
and lead optimization processes have shifted the chemical libraries toward poorer …
A general strategy for the synthesis of difluoromethyl-containing pyrazoles, pyridines and pyrimidines
VO Iaroshenko, V Specowius, K Vlach… - Tetrahedron, 2011 - Elsevier
Difluoromethyl-containing heteroannulated pyridines, pyrimidines and pyrazoles are
prepared by a two step method. The regioselective cyclizations of electron-excessive …
prepared by a two step method. The regioselective cyclizations of electron-excessive …
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists
AC Allan, A Billinton, SH Brown, A Chowdhury… - Bioorganic & medicinal …, 2011 - Elsevier
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists -
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ScienceDirect Skip to main contentSkip to article Elsevier logo Journals & Books Search …
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere
JD Downey, SA Saleh, TM Bridges, RD Morrison… - Bioorganic & medicinal …, 2013 - Elsevier
Recent preclinical studies demonstrate a role for the prostaglandin E2 (PGE2) subtype 1
(EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and …
(EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and …