20772-12-7Relevant articles and documents
Regiospecific synthesis of unsymmetrical α-bromoketones
Boyd,Rasmussen,Press
, p. 1045 - 1051 (1995)
A convenient regiospecific preparation of unsymmetrical α-bromoketones, commencing from Meldrum's acid, has been developed. This procedure allows for preparation of α-bromoketones which are unobtainable in a pure state by other bromination methods and is
PYRROLO [2,3-B]PYRIDINE-3-CARBOXAMIDE COMPOSITIONS AND METHODS FOR AMELIORATING HEARING LOSS
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, (2021/08/13)
N-(3-Substituted thiazol-2(3H)-ylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamides and N-(3-substituted oxazol-2(3H)-ylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamides (I) and (II) are disclosed. The compounds activate Yap and inhibit Lats kinases. They are therefore useful for treating hearing loss.
Design, synthesis, SAR and biological investigation of 3-(carboxymethyl)rhodanine and aminothiazole inhibitors of Mycobacterium tuberculosis Zmp1
Mori, Mattia,Deodato, Davide,Kasula, Mohan,Ferraris, Davide M.,Sanna, Adriana,De Logu, Alessandro,Rizzi, Menico,Botta, Maurizio
supporting information, p. 637 - 641 (2018/02/06)
Sixteen 3-(carboxymethyl)rhodanines, and twelve aminothiazoles as rhodanine-mimetics were designed, synthesized and tested as inhibitors of the Zmp1 enzyme from Mycobacterium tuberculosis (Mtb). Almost all rhodanines (5a–d, 5f–n, and 7a–b) exhibited Zmp1 inhibition with IC50 values in the range 1.3–43.9 μM, whereas only aminothiazoles 12b and 12d proved active with IC50 values of 41.3 and 35.7 μM, respectively. Structure-activity relationships (SAR) were coupled with molecular modeling studies to highlight structural determinants for Zmp1 inhibition. Moreover, rhodanines 5a and 5c induced 23.4 and 53.8% of Mtb growth inhibition in THP-1 infected cells, respectively, at the non-toxic concentration of 10 μg/ml. This work represents a step forward in targeting Zmp1 by small molecules.