223429-10-5Relevant academic research and scientific papers
Design and synthesis of novel metalloproteinase inhibitors
Nakatani, Shingo,Ikura, Masahiro,Yamamoto, Shingo,Nishita, Yoshitaka,Itadani, Satoshi,Habashita, Hiromu,Sugiura, Tsuneyuki,Ogawa, Koji,Ohno, Hiroyuki,Takahashi, Kanji,Nakai, Hisao,Toda, Masaaki
, p. 5402 - 5422 (2007/10/03)
A series of N-benzoyl 4-aminobutyric acid hydroxamate analogs were synthesized and evaluated as matrix metalloproteinase inhibitors. Synthetic work was focused on the chemical modification of the 4-aminobutyric acid part using easily available starting materials. As such, chemical modification was carried out using commercially available starting materials such as 4-aminobutyric acid, (+)- and (-)-malic acid, and d- and l-glutamic acid derivatives. Among the compounds tested, N-[4-(benzofuran-2-yl)benzoyl] 4-amino-4S-hydroxymethylbutyric acid hydroxamates derived from l-glutamic acid demonstrated more potent inhibitory activity against MMP-2 and MMP-9 compared with the corresponding 2S-hydroxy analogs or 3S-hydroxy analogs, respectively, which were derived from (-)-malic acid. Structure-activity relationship study is presented.
Total Synthesis of Microsclerodermin E
Zhu, Jidong,Ma, Dawei
, p. 5348 - 5351 (2007/10/03)
Succumbing to total synthesis: Microsclerodermin E, a 23-membered cyclic hexapeptide possessing antifungal activity, has been prepared for the first time. Key features in the synthesis include the construction of four unusual amino acid units, the assembl
Construction of three building blocks for the total synthesis of microsclerodermins
Sasaki, Shigekazu,Hamada, Yasumasa,Shioiri, Takayuki
, p. 453 - 455 (2007/10/03)
Three building blocks 2, 3, and 4 for the total synthesis of microsclerodermins (1) have been efficiently constructed from carboxylic acids 6, 14, and 20, respectively.
