Results 81 to 90 of about 1,668 (161)

Synthesis and biological evaluation of antiparasitic Cysteine protease inhibitors based on the Isatin Scaffold [PDF]

, 2004
Includes bibliographical references.Widespread drug resistance, loss of efficacy and toxicity has limited the full utilization of the current available drugs against malaria and other parasitic diseases.
Chiyanzu, Idan
core  

Thirty Years in the Design and Development of Cruzain Inhibitors

Journal of the Brazilian Chemical Society
Cruzipain is the principal protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Since its discovery in the 1980s and the resolution of the crystal structure of cruzain (a truncated recombinant form of the enzyme) in 1995, this target has attracted the interest of many research groups for screening studies, structure-based and ligand ...
Gabriel Jasinski, María Florencia Martini, Albertina Moglioni   +2 more
openaire   +2 more sources

Antiprotozoal quinolines containing electrophilic moieties [PDF]

, 2004
Includes bibliographical references.Compounds containing the quinoline moiety have been the mainstay of antimalarial chemotherapy. However, the emergence of resistant strains of Plasmodium falciparum, the causative agent of malaria, has compromised the ...
Ganto, Mlungiseleli Macdonald
core  

Cruzain [PDF]

Science-Business eXchange, 2008
openaire   +1 more source

Evaluating Known Zika Virus NS2B-NS3 Protease Inhibitor Scaffolds via In Silico Screening and Biochemical Assays. [PDF]

Pharmaceuticals (Basel), 2023
Santos LH, Rocha REO, Dias DL, Ribeiro BMRM, Serafim MSM, Abrahão JS, Ferreira RS.   +6 more
europepmc   +1 more source

Thermodynamic Drivers of Covalent Cruzain Inhibition Beyond Enthalpy-Entropy Compensation

Cysteine proteases are pivotal enzymes involved in diverse physiological and pathological processes, with cruzain and human cathepsin L emerging as key therapeutic targets. We report the design, synthesis, and characterization of a series of dipeptidyl inhibitors incorporating engineered modifications at the P1, P2, and P3 positions.
Luiz Fernando Barbosa, Fabiana Rossini, Evelin Ribeiro Cardoso, Felipe Cardoso Prado Martins, Carlos Alberto Montanari   +4 more
openaire   +1 more source

Machine Learning-Guided Repositioning of a SARS-CoV-2-Targeting Molecular Series as Cruzain Inhibitors. [PDF]

ChemMedChem
Lameiro RF, Barbosa LF, Cardoso ER, Ho BS, Martins FCP, de Melo BC, Rosini F, Shamim A, Souza PM, de Souza WF, Montanari CA.   +10 more
europepmc   +1 more source

Synthesis and Biological Evaluation of Tetrahydroisoquinoline Derivatives as Trypanocidal Agents. [PDF]

ACS Omega
de Moura Lopes JP, Marques GVL, Diniz LA, Côrrea Santos V, Resende DM, Murta SMF, Kohlhoff M, Maltarollo VG, Ferreira RS, Oliveira RB.   +9 more
europepmc   +1 more source

Haemanthidine-Containing Alkaloid Fraction from <i>Crinum scabrum</i> as a Natural Therapeutics for Chagas Disease. [PDF]

ACS Omega
Pardo JB, Orlando LMR, Lara LDS, Pereira MCS, de Sousa NF, Scotti L, Scotti MT, Borges WS.   +7 more
europepmc   +1 more source

Nitriles: an attractive approach to the development of covalent inhibitors. [PDF]

RSC Med Chem, 2023
Bonatto V, Lameiro RF, Rocho FR, Lameira J, Leitão A, Montanari CA.   +5 more
europepmc   +1 more source