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Changing substituent position revealed a more promising compound series of anti-inflammatory agents.
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In this paper, we present the pharmacological evaluation of a five-compound series of (4R -alkyl Glu analogs (1b–e,g) which may be envisaged as conformationally released designs of ATPA and 4R -alkylenes 2a–h.
Using 1400W [N- 3-aminomethylbenzyl)acetamidine], thiocitrulline and Nδ-(4,5-dihydrothiazol-2-yl)ornithine as lead compounds, series of N-benzyl- and N-phenyl-2-amino-4,5-dihydrothiazoles and thioureas were designed as inhibitors of NOS.
Analysis of the whole data set identified eight compound series and seven singletons of interest (data not shown).
Thus, each A_MMS represents a set of compound series with structurally analogous cores.
Compared to existing approaches these drawings substantially simplify the visual analysis of large compound series.
Using sophoridine (1) as the lead compound, a series of new N-substituted sophoridinic acid derivatives were designed, synthesized and evaluated for their cytotoxicity.
Based on the newly identified hit compound 17a, three series of compounds were synthesized and evaluated for both HDAC1 inhibitory activity and cytotoxicity.
From compound 47, a series of compounds was prepared and tested for inhibition against LmPyK at concentrations of 1 mM.
From compound 18, a series of compounds was synthesized and tested against TbPFK at 1 μM concentrations.
The g_ g conformers are found to be the most populated minima within the series of nonfluorinated compounds (series a), with significant amounts of pl conformers.
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