- 2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
-
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
- -
-
Page/Page column 211
(2021/06/26)
-
- Kinetics of the Reactions of Some 5-Bromo-2-nitro-3-R-thiophens, 3,4-dibromo-2-nitro-5-R-thiophens, 3-Bromo-2-nitro-5-R-thiophens, and 2-Bromo-3-nitro-5-R-thiophens with Nucleophiles in Methanol
-
The reactivity of some 5-bromo-2-nitro-3-R-thiophens (Ia-g; R=H, Me, Et, Prn, n-hexyl, Pri, and But), 3,4-dibromo-2-nitro-5-R-thiophens (IIa and b; R=H and Me), 3-bromo-2-nitro-5-R-thiophens (IIIa and b; R=H and Me), and 2-bromo-3-nitro-5-R-thiophens (IVa and b; R=H and Me) with amines and sodium benzenethiolate has been studied in methanol at various temperatures.Piperidinodebromination of compounds (Ia and c) has also been studied in benzene, in dioxan, and in dioxan-water (60:40 and 10:90).Independent of the position of the alkyl group (meta or para with respect to the leaving bromine), an unexpected alkyl activation has been observed, which represents a further exception to the electron-releasing behaviour of alkyl groups.
- Consiglio, Giovanni,Spinelli, Domenico,Gronowitz, Salo,Hoernfeldt, Anna-Britta,Maltesson, Britta,Noto, Renato
-
p. 625 - 630
(2007/10/02)
-