The straightforward conversion of alcohols to tertiary or secondary amines employing Nms‐amides in a single operation is described. The transformation features broad functional group tolerance and high stereospecificity, underscoring its utility in the synthesis of isotope‐labeled pharmaceuticals.
Jakub Brześkiewicz +3 more
wiley +1 more source
A Systematic Study of Auxochrome Effects on Fluorescence Under Conditions of Varying Temperature, pH, or Viscosity: Photo-induced electron transfer and Twisted Intramolecular Charge Transfer. [PDF]
Bibi A, Puntorieri R, Wheeler S.
europepmc +1 more source
Multitarget Drug Design for Cardiovascular Disease: Bridging Chemistry and Medicine
Many pathophysiological pathways associated with cardiovascular diseases involve multiple drug targets. This article reviews recent advances in the development of pharmacological compounds capable of simultaneously modulating multiple mechanisms. Multitarget drugs offer a promising therapeutic approach for complex cardiovascular disorders, including ...
Gyuzel Y. Mitronova +3 more
wiley +1 more source
Scaffold Hopping Provides Liver X Receptor Agonist With Preference for the β Subtype
A scaffold hopping strategy was pursued to enhance the binding pocket engagement and β‐subtype selectivity of liver X receptor agonist 2. The resulting spirocyclic lead compound, (S)‐7, demonstrates superior potency, enhanced potency‐based selectivity for LXRβ, and improved microsomal stability over the existing scaffold.
Annette Kärcher +5 more
wiley +1 more source
The hidden severity of new psychoactive substances: clinical evidence from emergency and intensive care admissions in Taiwan. [PDF]
Liao PH +9 more
europepmc +1 more source
A synthetic approach toward symmetrically substituted 1,4-bis(cinnamyl)piperazines [PDF]
A three-step pathway has been designed for the preparation of symmetrically substituted 1,4-bis(cinnamyl)piperazines starting from β-amino ketones. The approach comprises the bis-N-alkylation of piperazine with hydrochlorides of dimethylamine-based ...
Balan-Porcărașu, Mihaela +1 more
core
Hit‐to‐lead optimization of morpholinephenylbenzamides reveals key structure–activity relationships against Trypanosoma cruzi and Leishmania infantum. Potency, selectivity, and ADME properties are differentially improved across the series, identifying compounds 20, 24, and 16 as complementary templates for the future design of dual antiparasitic leads.
Danilo Nascimento Farago +15 more
wiley +1 more source
Structural Exploitation of Cinnarizine Identified Novel Drug-Like Anthelmintic Agents Against <i>Angiostrongylus cantonensis</i>. [PDF]
Lemes BL +7 more
europepmc +1 more source
Can simple linker descriptors guide PROTAC design? Analysis of matched CRBN‐ and VHL‐recruiting degraders shows that basic 2D linker properties may capture trends linked to degradation efficiency, in vitro ADME and physicochemical properties. A practical approach to reduce trial‐and‐error in early targeted protein degradation programs. Targeted protein
Giulia Apprato +3 more
wiley +1 more source
Synthesis of Sulfonamides in the Biobased Solvent Cyrene. [PDF]
Galli M +6 more
europepmc +1 more source

