99853-21-1Relevant articles and documents
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00677, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Deciphering Structure–Activity Relationships in a Series of 2,2-Dimethylchromans Acting as Inhibitors of Insulin Release and Smooth Muscle Relaxants
Pirotte, Bernard,Florence, Xavier,Goffin, Eric,Lebrun, Philippe
, p. 1810 - 1817 (2017/10/30)
4,6-Disubstituted 2,2-dimethylchromans are reported as pharmacologically active compounds that mainly target the ATP-sensitive potassium channels. The present study is an attempt to characterize the impact of the nature of substituents introduced at the 4- and 6-positions of 2,2-dimethylchromans on their capacities to inhibit insulin release from pancreatic β-cells or to relax vascular smooth muscle cells, both biological responses that are supposed to reflect interaction with specific ion channels. From the core structure 4-amino-2,2-dimethylchroman, a progressive increase in the steric hindrance of the chemical functionalities introduced at the 4-position (amino, formamido, acetamido, arylureido/thioureido) and at the 6-position (amino, formamido, acetamido, alkoxycarbonylamino) led to a progressive magnification of the inhibitory effect on the insulin release process and, to a lesser extent, of the vasorelaxant activity. Moreover, the dextrorotatory enantiomer of 2,2-dimethylchroman compound 29 was more potent than its levorotatory counterpart for inhibiting the insulin secretory process. Additional pharmacological investigations suggested, however, that the myorelaxant activity of 11 and 15 resulted from a direct Ca2+ entry blockade.
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors
Ng, Raymond A.,Sun, Minghua,Bowers, Simeon,Hom, Roy K.,Probst, Gary D.,John, Varghese,Fang, Lawrence Y.,Maillard, Michel,Gailunas, Andrea,Brogley, Louis,Neitz, R. Jeffrey,Tung, Jay S.,Pleiss, Michael A.,Konradi, Andrei W.,Sham, Hing L.,Dappen, Michael S.,Adler, Marc,Yao, Nanhua,Zmolek, Wes,Nakamura, David,Quinn, Kevin P.,Sauer, John-Michael,Bova, Michael P.,Ruslim, Lany,Artis, Dean R.,Yednock, Ted A.
, p. 4674 - 4679 (2013/08/23)
The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1′ region provided selectivity over Cat-D with a series of 2,2-dioxo-isothiochromanes and optimi
