90771-96-3Relevant academic research and scientific papers
COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION
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, (2021/06/11)
The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.
New anti-viral drugs for the treatment of the common cold
Maugeri, Caterina,Alisi, Maria A.,Apicella, Claudia,Cellai, Luciano,Dragone, Patrizia,Fioravanzo, Elena,Florio, Saverio,Furlotti, Guido,Mangano, Giorgina,Ombrato, Rosella,Luisi, Renzo,Pompei, Raffaello,Rincicotti, Vito,Russo, Vincenzo,Vitiello, Marco,Cazzolla, Nicola
, p. 3091 - 3107 (2008/09/20)
Human Rhinovirus (HRV) is the most important aetiologic agent of common cold in adults and children. HRV is a single-stranded, positive sense RNA virus and, despite the high level of conservation among different serotypes, sequence alignment of viral protease 3C with mammalian protease reveals no homology. Thus, protease 3C is an optimal target for the development of anti-HRV agents. In the present work we investigated the design, the synthesis and the development of new potential reversible inhibitors against HRV protease 3C. Docking studies on the crystallized structure of HRV2 protease 3C led us to the design and the synthesis of a series of 3,5 disubstituted benzamides able to act as analogues of the substrate. We also developed 1,3,5 trisubstituted benzamides where aromatic substitutions on the aryl ring led us to investigate the importance of π-π interaction on the stabilization of protease 3C-inhibitor complex. All structures were tested for enzymatic inhibition on HRV14 protease 3C. Results highlighted the inhibitory activity of compounds 13, 14, and 20 (91%, 81%, and 85% at 10 μM, respectively), with the latter exhibiting an ID50 (dose that inhibits 50% of the viral cytopathic effect) on HRV-14 = 25 μg/ml.
Enehydrazines, 36. Reaction of Enehydrazines with Acetylenecarboxylic Esters and 3-Butyn-2-one
Sucrow, Wolfgang,Turnschek, Wolfgang,Wolf, Ulrich,d'Amour, Hedwig,Krueger, Carl
, p. 1620 - 1635 (2007/10/02)
The enehydrazine-hydrazone tautomers 1 and 4 are added to dimethyl acetylenedicarboxylate and 8 to methyl propiolate to give the open-chain methyl 5-(2,2-dimethylhydrazino)pentadienoates 3, 5a, b and 9.The reactions of methyl propiolate and 3-butyn-2-one
