Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Synthesis of Arylpiperazine-Based CNS Ligands: Batch Disconnections and Their Continuous-Flow Implementation. [PDF]
Jeong D +5 more
europepmc +1 more source
Recent Advances in Biogas Production and Upgrading Technologies for Sustainable Energy Systems
Biogas technology is evolving from waste treatment into an intelligent renewable energy platform. Recent advances in anaerobic digestion, pretreatment, reactor design, biomethane upgrading, and AI‐driven process control improve methane recovery, stability, and gas purity.
Temechew Dessie +2 more
wiley +1 more source
Revisiting the Fragmentation of Ketoconazole by Positive Electrospray Ionization Tandem Mass Spectrometry and Density Functional Theory Calculations. [PDF]
Carnevale Neto F, Vessecchi R.
europepmc +1 more source
Studies of some novel piperazine derived amphiphiles and polymeric materials
This thesis describes the study of some novel piperazine derived amphiphiles and polymeric materials.Master of ...
Roshan Deen G.
core
Elucidating the Molecular Impact of DA29‐Induced ClpP Chemoactivation on Mitochondrial Function
A promising approach to tackling DIPG, a lethal pediatric brain tumor, relies on small molecules capable of activating the human mitochondrial protease hClpP. The novel piperazine‐based compound DA29 specifically activates endogenous hClpP, thereby compromising mtDNA levels, mitoribosomes, and OXPHOS complex subunits.
Francesca Rizzo +5 more
wiley +1 more source
40 years later: completion of the structural characterization of the anxiolytic drug buspirone HCl and solid-form landscape expansion. [PDF]
Botes DS +4 more
europepmc +1 more source
A series of 12 novel fused [6,6] saturated and unsaturated nitrogen bicycles is synthesized in three to five steps and expands the CRAFT library's fragment space. A 2,6‐naphthyridin‐3‐ol core replaces the dihydroquinolinone scaffold of aripiprazole, a scaffold‐hopping strategy.
Temitayo Omowumi Alegbejo Price +12 more
wiley +1 more source
1,2,3-Triazolyl indole-piperazine hybrids as potential anti-tubercular agents: design, synthesis, <i>in vitro</i>, and <i>in silico</i> evaluation. [PDF]
Reddyrajula R +7 more
europepmc +1 more source
Die direkte Umwandlung von Alkoholen in tertiäre oder sekundäre Amine in einem Reaktionsschritt unter Verwendung von Nms‐Amiden wird beschrieben. Die Transformation zeichnet sich durch eine breite Toleranz gegenüber verschiedenen funktionellen Gruppen und eine hohe Stereospezifität aus, was ihre Eignung für die Synthese isotopenmarkierter Arzneimittel ...
Jakub Brześkiewicz +3 more
wiley +1 more source

