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Biomedical subjects

S X Peng

Publications and source records attributed to S X Peng.

47 records · Page 3Linked to original sources

[Synthesis and antibacterial activity of 1-substituted benzyl quinolone acid derivatives].

The compounds of quinolone class, which were studied extensively and developed very quickly in the last decades, showed high activity, low toxicity and broad antibacterial spectrum. About thirty new compounds of 1,7-disubstituted-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids were synthesised and evaluated in vitro against S. aureus 25923, E. coli-25922 and P. aeruginosa. Their activities were low. The minimum inhibitory concentrations (MIC microgram/ml) of these compounds against Gram-positive bacteria were higher than those against Gram-negative bacteria. The relative in vitro activity contributed by 1-benzyl was: benzyl greater than p-chlorobenzyl greater than p-nitrobenzyl groups.

4-Quinolones↗

[Synthesis of N-(2-mercaptopyridyl-3-formyl)-N-alkyl glycine and the corresponding disulfides].

N-(2-mercaptopyridyl-3-formyl)-N-alkyl glycine I1-8) were synthesized by the condensation of 2-mercaptopyridyl-3-formyl chloride with ethyl N-alkyl glycinate followed by hydrolysis. The corresponding disulfides (II1-7) were obtained by the oxidation of compounds I1-7 with hydrogen peroxide (1%) in weak alkali medium below 10 degrees C. In preliminary tests, some compounds showed inhibitory activity of ACE in vitro.

Angiotensin-Converting Enzyme Inhibitors↗

Benzylisoquinoline compounds inhibit the ability of calmodulin to activate cyclic nucleotide phosphodiesterase.

Benzylisoquinoline compounds antagonised the ability of calmodulin (CaM) to stimulate the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase (CaM-PDE). This 'anti-CaM' activity was related to the hydrophobicity of the non-polar terminal region of the antagonist molecule. Antagonistic potency increased with the increase of hydrophobicity; the anti-CaM activity did not change when the polar terminus was a tertiary amine or quarternary amine. The anti-CaM potency was greater for bisbenzylisoquinoline compounds than for monobenzylisoquinoline compounds. Among the bisbenzylisoquinoline compounds anti-CaM pathway was: D3 greater than D2 berbamine greater than daurisoline greater than dauricine. Compound D3, which exhibited an IC50 value of 2.8 microM, was one of the most potent calmodulin antagonists, among benzylisoquinoline compounds, so far reported.

2',3'-Cyclic-Nucleotide Phosphodiesterases↗