Simulation of the Metabolism of New Psychoactive Substances Using Electrochemistry-Mass Spectrometry: Introducing an Innovative Software Tool for Rapid Data Evaluation. [PDF]
A novel software tool for the rapid and efficient simulation of the metabolism of new psychoactive substances was developed and applied to mimic the metabolism of the synthetic cannabinoid receptor agonist MDMB‐4en‐PINACA. ABSTRACT An innovative software tool for the rapid and efficient simulation of the metabolism of new psychoactive substances (NPS ...
Wesner M +3 more
europepmc +2 more sources
Photoenzymatic Hydroalkylation Enables Streamlined Access to Aryl Glutarimide Precursors. [PDF]
We report a photoenzymatic hydroalkylation that enables streamlined, stereocontrolled access to aryl glutarimide precursors relevant to targeted protein degradation. Engineered flavin‐dependent “ene”‐reductases provide broad scope and high enantioselectivity through a distinct electron transfer–enantioselective proton transfer pathway.
Xu Z +9 more
europepmc +3 more sources
Recent Advances in Indazole-Containing Derivatives: Synthesis and Biological Perspectives
Indazole-containing derivatives represent one of the most important heterocycles in drug molecules. Diversely substituted indazole derivatives bear a variety of functional groups and display versatile biological activities; hence, they have gained ...
Shu-Guang Zhang +2 more
doaj +1 more source
Regioselective zincation of indazoles using TMP2Zn and Negishi cross-coupling with aryl and heteroaryl iodides. [PDF]
The metalation of various SEM-protected functionalized indazoles with TMP2Zn provides 3-zincated indazoles which undergo palladium-catalyzed Negishi cross-couplings in good ...
Andreas Unsinn +40 more
core +1 more source
Pd(PPh3)4 Catalyzed Synthesis of Indazole Derivatives as Potent Anticancer Drug
A series of 3-aryl indazoles and 1-methyl-3-aryl indazole derivatives are prepared with exceptional yields by coupling with several arylboronic acids and methylation by two dissimilar approaches.
Jagan Mohana Rao Saketi +7 more
doaj +1 more source
Lead identification and structure-activity relationships of heteroarylpyrazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists [PDF]
A knowledge-based library of aryl 2,3-dichlorophenylsulfonamides was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme.
Copley, R.C.B. +4 more
core +1 more source
Rhodium(I) indazole and indazolate complexes
The preparation of cationic indazole (HIdz) rhodium(I) complexes of the types [(diolefin)Rh(HIdz)2]ClO4 and [(CO)2Rh(HIdz)2]ClO4 is described. Neutral binuclear rhodium(I) complexes of the type [Y2Rh(μ-Idz)]2 (Y2 = COD, TFB, NBD, (CO)2 or (CO)(PPh3)) are obtained by treating the corresponding complexes [Y2RhCl]2 with indazole and organic or inorganic ...
Usón, Rafael +3 more
openaire +2 more sources
Discovery of orexant and anorexant agents with indazole scaffold endowed with peripheral antiedema activity [PDF]
CB1 receptors and endocannabinoids are integrated components of neuronal networks controlling different organism’s functions, such as appetite and food intake in the hypothalamus.
Dimmito, Marilisa P. +7 more
core +2 more sources
Unusual DNA binding modes for metal anticancer complexes [PDF]
DNA is believed to be the primary target for many metal-based drugs. For example, platinum-based anticancer drugs can form specific lesions on DNA that induce apoptosis.
Pizarro, Ana M., Sadler, P. J.
core +1 more source
Synthesis and Cytotoxic Activity of Combretastatin A-4 and 2,3-Diphenyl-2H-indazole Hybrids
Cancer is the second leading cause of death, after cardiovascular diseases. Different strategies have been developed to treat cancer; however, chemotherapy with cytotoxic agents is still the most widely used treatment approach.
Jaime Pérez-Villanueva +11 more
doaj +1 more source

