Results 181 to 190 of about 81,237 (352)

Allosteric Inhibitors of SARS‐CoV‐2 RNA‐Dependent RNA Polymerase Based on N,N′‐Diphenylurea

ChemMedChem, Volume 21, Issue 1, January 2026.
Inhibitors of SARS‐CoV‐2 RdRp activity based on N,N′‐diphenylurea scaffold have been identified. Several compounds exhibit residual activity (RA) below 50% in an enzymatic assay (at 10 µM concentration) and improved aqueous solubility compared to the previously reported series of inhibitors.
Artem Chayka, Matěj Danda, Alžběta Dostálková, Vojtěch Spiwok, Lamija Zijadic, Anna Klimešová, Marina Kapisheva, Michala Zgarbová, Jan Weber, Tomáš Ruml, Michaela Rumlová, Zlatko Janeba   +11 more
wiley   +1 more source

Editorial: Recent advances in synthesizing and utilizing nitrogen-containing heterocycles

Frontiers in Chemistry
Takashi Ohshima, Hsyueh-Liang Wu, Hyun-Joon Ha   +2 more
doaj   +1 more source

Optimization of 4‐Amino‐2‐Pyridone Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9: Integrating Structure–Activity and Structure–Metabolism Relationships

ChemMedChem, Volume 21, Issue 1, January 2026.
Green chemistry‐based late‐stage functionalization (LSF) of the anti‐proprotein convertase subtilisin/kexin type 9 (PCSK9) early lead compound 5c led to optimized analogs with improved metabolic stability/PCSK9 IC50 ratio. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key drug target for the treatment of different hypercholesterolemia ...
Lisa Giannessi, Maria Giovanna Lupo, Martina Ugolotti, Bianca Papotti, Beatrice Mattina, Maria Grazia Martina, Anna Demurtas, Cristina Padula, Sara Nicoli, Marco Crescenzio, Nicola Ferri, Francesca Zimetti, Marco Radi   +12 more
wiley   +1 more source

Ligand flexibility as a concept to unlock catalytic activity: acyclic carbenes for base-free transfer ruthenium hydrogenation catalysis. [PDF]

Chem Sci
Righetti G, Koidan G, Filimonchuk SL, Shishkina S, Kostyuk A, Albrecht M.   +5 more
europepmc   +1 more source

A modular and divergent approach to spirocyclic pyrrolidines

, 2020
Benjamin D. A. Shennan, P. W. Smith, Yusuke Ogura, Darren J. Dixon   +3 more
openalex   +2 more sources

Synthesis and In Vitro Activity of Hypofuran B and Analogs Against Plasmodium Falciparum and Trypanosoma Cruzi

ChemMedChem, Volume 21, Issue 1, January 2026.
Hypofuran B, drynaran, and a series of analogs are obtined by crossed aldol condensation from furfural dereivatives. Compunds are tested for in vitro activity agaisnt Trypanosoma cruzi and Plasmodium falciparum. Best results are obtained Against P. falciparum, with IC50 values ranging from 5,35 to 10,35 µg mL−1.
Cristiane Aparecida Franco, Jodieh Oliveira Santana Varejão, Isabela Penna Ceravolo, Victória Miranda Machado, Antoniana Ursine Krettli, Daniela de Melo Resende, Silvane Maria Fonseca Murta, Felipe Terra Martins, Eduardo Jorge Pilau, Vinícius Ribeiro Montes, Markus Kohlhoff, Eduardo V. V. Varejão   +11 more
wiley   +1 more source

Scaffold Simplification Yields Potent Antibacterial Agents That Target Bacterial Topoisomerases. [PDF]

Molecules
Khudiakova L, Komarova K, Zhuravlev M, Deniskin D, Golovanov A, Nichugovskiy A, Babkin K, Zakharova M, Chudinov M, Rogacheva E, Kraeva L, Shevtsova O, Ipatova D, Skvortsov D, Lukianov D, Kryakvin M, Gureev M, Lukin A.   +17 more
europepmc   +1 more source

Locked Conformations for Proline Pyrrolidine Ring:  Synthesis and Conformational Analysis of cis- and trans-4-tert-Butylprolines

, 2005
Ari M. P. Koskinen, Juho Helaja, Esa T. T. Kumpulainen, Jari Koivisto, H. Mansikkamaki, Kari Rissanen   +5 more
openalex   +2 more sources

Exploration and Characterization of the Antimalarial Activity of Pyrimidine‐2,4‐Diamines for which Resistance is Mediated by the ABCI3 Transporter

ChemMedChem, Volume 21, Issue 1, January 2026.
Investigation of the structure‐activity relationship on W482 (1) with a pyrimidine‐2,4‐diamine scaffold culminated in analog 51 with enhanced anti‐plasmodial activity. Forward genetics and phenotypic examination revealed the ABCI3 transporter protein as a putative resistance mechanism.
Mahta Mansouri, Madeline G. Dans, Zijun Low, Katie Loi, Kate E. Jarman, Jocelyn S. Penington, Deyun Qiu, Adele M. Lehane, Benigno Crespo, Franciso‐Javier Gamo, Delphine Baud, Stephen Brand, Paul F. Jackson, Alan F. Cowman, Brad E. Sleebs   +14 more
wiley   +1 more source

An Fe(II)-catalyzed synthesis of spiro[indoline-3,2'-pyrrolidine] derivatives. [PDF]

Beilstein J Org Chem
Gradova EV, Ozhegov NA, Shcherbakov RO, Tkachenko AG, Nesterova LY, Mendogralo EY, Uchuskin MG.   +6 more
europepmc   +1 more source