132991-46-9

Upstream product

• 1015083-66-5 C₁₉H₂₃NO₂ 
• 939-97-9 4-tert-Butylbenzaldehyde 
• 150-13-0 4-amino-benzoic acid 
• 1608118-59-7 4-(4-tert-butylbenzylideneimino) benzoic acid 

Downstream Products

• 1246560-51-9 [4-(4-tert-butylbenzylamino)phenyl](4-methoxyphenyl)methanone 
• 1246560-47-3 [4-(4-tert-butylbenzylamino)phenyl]-p-tolylmethanone 
• 1246560-55-3 [4-(4-tert-butylbenzylamino)phenyl](2,4-dimethoxyphenyl)methanone 

Relevant academic research and scientific papers

Carbonic anhydrase inhibitors. Inhibition of human cytosolic isoforms i and II with (reduced) Schiff's bases incorporating sulfonamide, carboxylate and carboxymethyl moieties

A library of Schiff bases was synthesized by condensation of aromatic amines incorporating sulfonamide, carboxylic acid or carboxymethyl functionalities as Zn2+-binding groups, with aromatic aldehydes incorporating tert-butyl, hydroxy and/or methoxy groups. The corresponding amines were thereafter obtained by reduction of the imines. These compounds were assayed for the inhibition of two cytosolic human carbonic anhydrase (hCA, EC 4.2.1.1) isoenzymes, hCA I and II. The Ki values of the Schiff bases were in the range of 7.0-21,400 nM against hCA II and of 52-8600 nM against hCA I, respectively. The corresponding amines showed Ki values in the range of 8.6 nM-5.3 μM against hCA II, and of 18.7-251 nM against hCA I, respectively. Unlike the imines, the reduced Schiff bases are stable to hydrolysis and several low-nanomolar inhibitors were detected, most of them incorporating sulfonamide groups. Some carboxylates also showed interesting CA inhibitory properties. Such hydrosoluble derivatives may show pharmacologic applications.

Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein inhibitors

Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previosuly-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 μM.