Synthesis and Neurotrophic Activities of N‐p‐Tolyl/phenylsulfonyl L‐Amino Acid Thiolester Derivatives

Abstract

Various N-p-tolyl/phenylsulfonyl L-amino acid thiolester derivatives were designed and synthesized according to combination of functional groups. The synthesized compounds were identified by spectral methods ( 1 H NMR, 13 C NMR, MS and HRMS). Preliminary bioassays indicated that the compounds 4a, 4b, 4d, 5c, 5d, 5g, 6b and 6dshowed remarkable activities and the compounds 4c, 5b and 6c showed moderate activities to inhibit anoxic damage of PC12 cells at 10 µg/mL, but the compounds 4d and 6d only showed moderate protective activities against PC12 cells at 5 µg/mL. Preliminary bioassays also indicated that the compounds 4c, 5a, 5c, 5d, 5e and 6b showed moderate activities to induce PC12-differentiation at 10 µg/mL.

Determination of lactate dehydrogenase isoenzymes in single rat glioma cells by capillary electrophoresis with electrochemical detection

“…8 min. The enzyme-catalyzed reaction caused by the LDH zone migrating in the capillary should be responsible for the plateau [15]. The peak on the curve 1 produced during the incubation, eluting at 13 min, could be identified as the peak of LDH on the basis of the migration time by comparing the NADH peak shown in curve 3. q was used to quantify.…”

Synthesis of Some new Sulfonamide Schiff’s Bases and Study Their Gastroprotective Activity

“…The mass spectra of Schiff bases (1-4) were measured and the fragmentation routes for these compounds were suggested, as shown in schemes (1)(2)(3)(4) .with the parent peaks at m/z 304,266,380,341 respectively. Table (5) shows the import ions that appear in the spectra of these compounds.…”

“…Schiff bases have been widely investigated and become one of the research hotspots for a long period of time owing to their strong coordination capability and diverse biological activities, such as antibacterial, antitumor activities, etc. [1][2][3]. Many Schiff bases are known to be medicinally important and used to design medicinal compounds [4][5][6][7].…”

A QSAR Study on Neurotrophic Activities of N-p-Tolyl/phenylsulfonyl L-Amino Acid Thiolester Derivatives

“…Yang et al (2008) [12] synthesized seventeen N-p-tolyl/phenylsulfonyl L-amino acid thiolester derivatives according to combination of functional groups (as shown in Fig.1 and TABLE I), and the protective effects of these target compounds on anoxic damage of rat pheochromocytoma (PC12) cells were also studied at drug concentration of 5, 10 and 20 ȝg mL -1 , respectively. The majority of these compounds showed remarkable or moderate neurotrophic activities, and thus they were selected for a QSAR study in the present work.…”

“…STRUCTURES OF THE TARGET COMPOUNDS AND PROTECTIVE EFFECTS OF LIVABILITY ON ANOXIC DAMAGE OF PC12 CELLS[12] .…”