Abeta aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides.
Phenylazo benzenesulfonamides were designed and synthesized as beta-amyloid (Abeta40) fibril assembly inhibitors, and evaluated for inhibition of Abeta40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe(2) group on the end of the phenylazo moiety may play an important role in preventing Abeta40 fibril formation. LB-152 provides a new lead for further development of potential beta-amyloid aggregation inhibitors to treat AD.
Department of Medicinal Chemistry, College of Pharmacy, Taipei Medical University, 250 Wu-Hsing St., Taipei 110, Taiwan.
Shwu-Jiuan
SJ
Lin
Young-Ji
YJ
Shiao
Chih-Wen
CW
Chi
Li-Ming
LM
Yang
D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000096926:Benzenesulfonamides
D016229:Amyloid beta-Peptides; D013449:Sulfonamides; D000096926:Benzenesulfonamides