Investigating the Ligand‐Binding Properties of N‐arylbenzimidazoles as Novel Elastase Inhibitors
A series of novel N‐[(3,5‐dimethylphenyl)methyl]‐1H‐benzimidazole derivatives is designed, synthesized, and evaluated for inhibitory activity against elastase. Several compounds demonstrate an antielastase activity, including the N‐(2‐bromophenyl)‐2‐(6‐chloro‐1‐(3,5‐dimethylbenzyl)‐1H‐benzo[d]imidazol‐2‐ylthio)acetamide, showing the greatest potency ...
Giovanna Pitasi +6 more
wiley +1 more source
A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova +15 more
wiley +1 more source
Cytotoxicity and Antimicrobial Activity of GaMF1 Analogs
GaMF1 is a reported, highly potent inhibitor of mycobacterial ATP synthase. Structural modification of this scaffold significantly changes biological activity. We present GaMF1 analogues with strong antiparasitic effects, potential antiproliferative properties, and discuss the selectivity limitations of the parent compound and its analogues.
Jan Chasák +8 more
wiley +1 more source
The "Click-tail approach" for the design and synthesis of novel carbonic anhydrase inhibitors [PDF]
The Carbonic Anhydrases (CAs) are a family of zinc enzymes deputed to the interconversion of carbonic dioxide to hydrogen carbonate. Herein, we report on a sustainable modular strategy, also called "clicktail approach", used to obtain two series of 4-(4 ...
Carta, Fabrizio +6 more
core
Direct‐to‐Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery
Crude yet clever: Direct‐to‐biology workflows exploit nanoscale synthesis and plate‐based assays to accelerate hit discovery, save precious intermediates, and rethink early drug discovery. Direct‐to‐biology (D2B) has emerged as a transformative concept in early drug discovery, defined by the direct on‐target screening of crude reaction mixtures without
Ariane F. Hübner, Fabian Barthels
wiley +1 more source
Association of mating-type with mycelium growth rate and genetic variability of Fusarium culmorum
Irzykowska Lidia +2 more
doaj +1 more source
Introducción: Lippia origanoides H.B.K. (Verbenacea), es una planta aromática conocida comúnmente como "orégano". Los aceites esenciales de 8 muestras de L.
Bibiana Zapata +4 more
doaj
Host Preference Associated With Deoxynivalenol and Nivalenol Chemotypes in Fusarium graminearum, F. asiaticum, and F. meridionale. [PDF]
Liu X +11 more
europepmc +1 more source
Long-term neighbor identity influences effectiveness of sagebrush responses to damage-induced volatiles of those neighbors. [PDF]
Shiojiri K +3 more
europepmc +1 more source
Assessing the Biogeographic Risks of Potentially Toxic Plants-A Case Study for a Novel Locoweed <i>Sphaerophysa salsula</i> in China. [PDF]
Zhang YY +4 more
europepmc +1 more source

