A.S.S. Domling

Despite its potential, it remains very much underutilized in medicinal chemistry. It was first described by Banfi et al. link.springer.com/article/10.102…

🌟 PADAM Reaction (Passerini reaction–Amine Deprotection–Acyl Migration) is a highly versatile multicomponent reaction (MCR) concept to the straightforward and efficient synthesis of complex protease inhibitors #MCR #ProteaseInhibitors #chemistry

Malaria active #isocyanide natural products pubs.acs.org/doi/10.1021/ac… and stereoselective synthesis of isocyanoterpene Pustulosaisonitrile-1 pubs.acs.org/doi/10.1021/ac…

Isocyanides in #Space : HNC, hydromagnesium isocyanide (HMgNC), and isocyano-diacetylene (HC4NC) and many more iopscience.iop.org/article/10.108… pubs.acs.org/doi/abs/10.102…

This innovative dual-target approach offers a promising strategy to combat resistance by targeting both a viral and a human protease, ensuring therapeutic efficacy even against emerging viral mutations. #COVID19Therapeutics #ProteaseInhibitors #drugdiscovery

X-ray structures revealed thiohemiacetal formation with Cys145 and critical hydrogen bonding in the active site of 3CL-PR, explaining the enhanced potency of 2-pyridon-3-yl-alanyl derivatives. #COVID19Therapeutics #ProteaseInhibitors #DrugDiscovery

pubs.acs.org/doi/10.1021/ja… Dual-Target Inhibitors Against SARS-CoV-2: We designed and synthesized dual-acting peptidomimetic aldehyde inhibitors targeting SARS-CoV-2 3CL protease (3CL-PR) and human cathepsin L (hCatL), key proteases in viral replication and infection.

β-Carbonyl radicals generated from cyclopropyl alcohols react with 2-(2-isocyanophenyl)acetonitriles, yielding #quinolin-3-amines undergoing intramolecular cyclization and dehydrogenation to form the final products. #Chemistry #OrganicChemistry #SyntheticChemistry #NHeterocycles

pubs.acs.org/doi/10.1021/ac… 🚀 Efficient N-Heterocycle Synthesis: Mn(III)-mediated domino cascade reaction for the synthesis of polysubstituted benzo[b][1,5]naphthyridines via C–C bond cleavage of cyclopropanols. #SyntheticChemistry #NHeterocycles #CascadeReactions

This study pioneers helix sense-selective living polymerization, producing uniaxially oriented solid polymer films via magnetic field alignment, highlighting the potential of CLCs for chiral polymer synthesis. #ChiralPolymers #LiquidCrystals #LivingPolymerization #ChemistryIsKey

Using CLC as a chiral solvent, the process imparts chirality to the PAIs, which exhibit a lyotropic twist-bend nematic phase (Ntb). #ChiralPolymers #LiquidCrystals #LivingPolymerization #ChemistryIsKey

pubs.acs.org/doi/abs/10.102… 🌟 **Living polymerization in chiral liquid crystals (CLC)** enables the synthesis of one-handed helical poly(aryl isocyanides) (PAIs) from achiral monomers with controlled molecular weights and narrow polydispersity.

potent D2 receptor binder by the beautiful interrupted #UgiReaction #DrugDiscovery #MedicinalChemistry #MulticomponentReactions #MCR #OrganicChemistry #Chemistry pubs.acs.org/doi/full/10.10…

Highly interesting study on the drug-likeness of #PasserinReaction products and their metabolic stability: important for both prodrugs, soft and hard #drugs pubs.acs.org/doi/abs/10.102… #DrugDiscovery #MedicinalChemistry #MulticomponentReactions #OrganicChemistry #Chemistry

Beautiful scaffolds: oxindole−β-lactam and oxindole−γ-lactam by #UgiReaction pubs.acs.org/doi/abs/10.102… #DrugDiscovery #MedicinalChemistry #MulticomponentReactions #OrganicChemistry #Chemistry

Despite misconceptions about their simplicity, MCRs accelerate the development of diverse, topologically rich chemotypes for medicinal chemistry, driving breakthroughs in clinical compound discovery. #DrugDiscovery #MedicinalChemistry #MulticomponentReactions

🔬 Multicomponent reactions (MCRs) are revolutionizing drug discovery by enabling the one-pot synthesis of complex molecules, including those with quaternary and chiral centers. #DrugDiscovery #MedicinalChemistry #MulticomponentReactions pubs.acs.org/doi/abs/10.102…

MraY inhibitors by Ugi reaction: pubs.acs.org/doi/full/10.10…

🌟 High atom economy, broad substrate scope, and great yields, great chemistry.

💡 Balalaie et al: A palladium-catalyzed domino reaction of isocyanides with 2H-azirines delivers tetrasubstituted pyrimidines in one pot via C–C and C–N bond formations!. #Chemistry #Catalysis #Innovation #Pyrimidines pubs.acs.org/doi/10.1021/ac…