Bioisosteres of the phenyl ring: recent strategic applications in lead optimization and drug design
MAM Subbaiah, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
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 …
Base‐Modulated 1, 3‐Regio‐and Stereoselective Carboboration of Cyclohexenes
W Kong, Y Bao, L Lu, Z Han, Y Zhong… - Angewandte Chemie …, 2023 - Wiley Online Library
While chain‐walking stimulates wide interest in both polymerization and organic synthesis,
site‐and stereoselective control of chain‐walking on rings is still a challenging task in the …
site‐and stereoselective control of chain‐walking on rings is still a challenging task in the …
Advances in the development of phosphodiesterase-4 inhibitors
T Peng, B Qi, J He, H Ke, J Shi - Journal of Medicinal Chemistry, 2020 - ACS Publications
Cyclic nucleotide phosphodiesterase 4 (PDE4) specifically hydrolyzes cyclic adenosine
monophosphate (cAMP) and plays vital roles in biological processes such as cancer …
monophosphate (cAMP) and plays vital roles in biological processes such as cancer …
Furazans in medicinal chemistry
RS Mancini, CJ Barden, DF Weaver… - Journal of Medicinal …, 2021 - ACS Publications
Incorporation of heterocycles into drug molecules can enhance physical properties and
biological activity. A variety of heterocyclic groups is available to medicinal chemists, many …
biological activity. A variety of heterocyclic groups is available to medicinal chemists, many …
Advances in the development of phosphodiesterase-4 inhibitors
G Li, D He, X Cai, W Guan, Y Zhang, JQ Wu… - European Journal of …, 2023 - Elsevier
Abstract Phosphodiesterase 4 (PDE4) hydrolyzes cyclic adenosine monophosphate (cAMP)
and plays a vital roles in many biological processes. PDE4 inhibitors have been widely …
and plays a vital roles in many biological processes. PDE4 inhibitors have been widely …
Design of a multi-target focused library for antidiabetic targets using a comprehensive set of chemical transformation rules
FI Saldívar-González, G Navarrete-Vázquez… - Frontiers in …, 2023 - frontiersin.org
Virtual small molecule libraries are valuable resources for identifying bioactive compounds
in virtual screening campaigns and improving the quality of libraries in terms of …
in virtual screening campaigns and improving the quality of libraries in terms of …
Optimizing solubility and permeability of a biopharmaceutics classification system (BCS) class 4 antibiotic drug using lipophilic fragments disturbing the crystal lattice
U Tehler, JH Fagerberg, R Svensson… - Journal of medicinal …, 2013 - ACS Publications
Esterification was used to simultaneously increase solubility and permeability of
ciprofloxacin, a biopharmaceutics classification system (BCS) class 4 drug (low solubility/low …
ciprofloxacin, a biopharmaceutics classification system (BCS) class 4 drug (low solubility/low …
Domino reaction of arylglyoxals with pyrazol-5-amines: selective access to pyrazolo-fused 1, 7-naphthyridines, 1, 3-diazocanes, and pyrroles
B Jiang, W Fan, MY Sun, Q Ye, SL Wang… - The Journal of …, 2014 - ACS Publications
New multicomponent domino reactions of arylglyoxals with pyrazol-5-amines have been
established, providing selective access to unprecedented pyrazolo-fused 1, 7 …
established, providing selective access to unprecedented pyrazolo-fused 1, 7 …
Design, synthesis and evaluation of 2-pyrimidinylindole derivatives as anti-obesity agents by regulating lipid metabolism
SY Guo, LY Wei, BB Song, YT Hu, Z Jiang… - European Journal of …, 2023 - Elsevier
Obesity, a global pandemic posing a growing threat to human health, necessitates the
development of effective and safe anti-obesity agents. Our previous studies highlighted the …
development of effective and safe anti-obesity agents. Our previous studies highlighted the …