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 …

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery

B Das, ATK Baidya, AT Mathew, AK Yadav… - Bioorganic & Medicinal …, 2022 - Elsevier
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 …

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 …

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 …

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 …

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 …

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 …

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 …

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 …

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 …