Results 31 to 40 of about 2,082 (147)

Synthesis and Biological Evaluation of Dantrolene‐Like Hydrazide and Hydrazone Analogues as Multitarget Agents for Neurodegenerative Diseases

ChemMedChem, Volume 16, Issue 18, Page 2807-2816, September 16, 2021., 2021
Simpler is better: Structural modifications of the chemical structure of dantrolene, previously disclosed as a repositionable drug with potential for Alzheimer's disease, allowed preparing new small molecules with multitarget activity profile. Compared to dantrolene, molecular simplification resulted in less toxic and more soluble compounds.
Isabella Bolognino, Nicola Giangregorio, Annamaria Tonazzi, Antón L. Martínez, Cosimo D. Altomare, María I. Loza, Sara Sablone, Saverio Cellamare, Marco Catto   +8 more
wiley   +1 more source

Stapled ACE2 peptidomimetics designed to target the SARS‐CoV‐2 spike protein do not prevent virus internalization

Peptide Science, Volume 113, Issue 4, July 2021., 2021
Abstract COVID‐19 is caused by a novel coronavirus called severe acute respiratory syndrome‐coronavirus 2 (SARS‐CoV‐2). Virus cell entry is mediated through a protein‐protein interaction (PPI) between the SARS‐CoV‐2 spike protein and angiotensin‐converting enzyme 2 (ACE2).
Danielle C. Morgan, Caroline Morris, Amit Mahindra, Connor M. Blair, Gonzalo Tejeda, Imogen Herbert, Matthew L. Turnbull, Gauthier Lieber, Brian J. Willett, Nicola Logan, Brian Smith, Andrew B. Tobin, David Bhella, George Baillie, Andrew G. Jamieson   +14 more
wiley   +1 more source

New platinum(II) complexes of cycloalkanespiro-5-(2-thiohydantoins). Synthesis and quantum chemical investigation

Acta Chimica Slovenica, 2015
Synthesis and characterization of new Pt(II) complexes of cyclohexanespiro-5-(2-thiohydantoin)  (L1) and cycloheptanespiro-5-(2-thiohydantoin) (L2) are discussed. The new complexes are studied by elemental analysis, IR, ATR FTIR spectroscopy.
Petja E. Marinova, Marin Marinov, Vassil Delchev, Neyko Stoyanov   +3 more
doaj   +1 more source

Protein Adductomics: Methodologies for Untargeted Screening of Adducts to Serum Albumin and Hemoglobin in Human Blood Samples. [PDF]

, 2019
The reaction products of electrophiles in vivo can be measured as adducts to the abundant proteins, hemoglobin (Hb), and human serum albumin (HSA), in human blood samples.
Carlsson, Henrik, Rappaport, Stephen, Törnqvist, Margareta   +2 more
core   +2 more sources

Cell‐Based Identification of New IDO1 Modulator Chemotypes

Angewandte Chemie, Volume 133, Issue 18, Page 9957-9962, April 26, 2021., 2021
Heme‐competitive indoleamine‐2,3‐dioxygenase (IDO1) small‐molecule modulators are under‐represented as heme displacement is delayed in in vitro assays. This limitation can be overcome by cell‐based screening as employed in this study, which revealed novel chemotypes that potently inhibit IDO1 activity and kynurenine production by competing with heme ...
Elisabeth Hennes, Philipp Lampe, Lara Dötsch, Nora Bruning, Lisa‐Marie Pulvermacher, Sonja Sievers, Slava Ziegler, Herbert Waldmann   +7 more
wiley   +1 more source

Necrostatin-1 Analogues: Critical Issues on the Specificity, Activity and In Vivo Use in Experimental Disease Models [PDF]

, 2012
Necrostatin-1 (Nec-1) is widely used in disease models to examine the contribution of receptor-interacting protein kinase (RIPK) 1 in cell death and inflammation.
Callewaert, N, Cauwels, A, Declercq, W, Degterev, A, DuHadaway, J B, Duprez, L, Goossens, V, Grootjans, S, Libert, C, Nerinckx, W, Prendergast, G C, Roelandt, R, Takahashi, N, Van Hauwermeiren, F, Vandenabeele, P, Yuan, Junying   +15 more
core   +2 more sources

Heterocyclic systems containing S/N regioselective nucleophilic competition: Facile synthesis, antitubercular and antimicrobial activity of thiohydantoins and iminothiazolidinones containing the benzo [PDF]

Journal of the Serbian Chemical Society, 2005
The required compounds N-aryl-N'-(3-chloro-2-benzo[b]thenoyl)-thioureas 1a-k were prepared by condensing 3-chloro-2-benzo[b]thenoyl chloride with different arylamines using ammonium thiocyanate, which in turn when treated with chloroacetic acid, yielded ...
Kachhadia V.V., Patel M.R., Joshi H.S.
doaj   +1 more source

Experimental and computational study of the energetics of hydantoin and 2-thiohydantoin [PDF]

, 2013
This work reports an experimental and a theoretical study of two imidazolidine derivatives, hydantoin (CAS No. 461-72-3) and 2-thiohydantoin (CAS No. 503-87-7).
Alvaro Cimas, Ana L R Silva, Manuel J S Monte, Maria D M C R Ribeiro da Silva, Nuno Vale, Paula Gomes   +5 more
core   +1 more source

Synthesis and antibacterial activity of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moieties

Saudi Pharmaceutical Journal, 2018
A series of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moiety (28–65) were synthesized by the reaction of (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid chlorides with 5 ...
Nazar Trotsko, Urszula Kosikowska, Agata Paneth, Monika Wujec, Anna Malm   +4 more
doaj   +1 more source

Glucose-derived spiro-isoxazolines are anti-hyperglycemic agents against type 2 diabetes through glycogen phosphorylase inhibition [PDF]

, 2016
International audienceGlycogen phosphorylase (GP) is a target for the treatment of hyperglycaemia in the context of type 2 diabetes. This enzyme is responsible for the depolymerization of glycogen into glucose thereby affecting the levels of glucose in ...
Azay-Milhau, Jacqueline, Balzarin, Sophie, Chajistamatiou, Aikaterini S., Chrysina, Evangelia D., Docsa, Tibor, Duret, Cédric, Gergely, Pál, Goyard, David, Kónya, Bálint, Leroy, Jérémy, Maurel, Patrick, Petit, Pierre, Praly, Jean-Pierre, Somsák, László, Tournier, Michel, Tousch, Didier, Vidal, Sébastien   +16 more
core   +2 more sources