2. Academic Validation
  3. Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase

Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase

  • Bioorg Med Chem Lett. 2004 May 3;14(9):2227-31. doi: 10.1016/j.bmcl.2004.02.011.
Gregory S Bisacchi 1,  William A Slusarchyk,  Scott A Bolton,  Karen S Hartl,  Glenn Jacobs,  Arvind Mathur,  Wei Meng,  Martin L Ogletree,  Zulan Pi,  James C Sutton,  Uwe Treuner,  Robert Zahler,  Guohua Zhao,  Steven M Seiler
Affiliations

Affiliation

  • 1 The Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. gregory.bisacchi@bms.com
PMID: 15081014 DOI: 10.1016/j.bmcl.2004.02.011
Abstract

Azetidinones such as BMS-363131 (2) and BMS-363130 (3), which contain a guanidine group in the C-3 side chain were previously shown to be very potent inhibitors of human tryptase with high selectivity versus Other serine proteases, including trypsin. In this letter, we describe the discovery of a number of potent azetidinone tryptase inhibitors in which the guanidine moiety at the ring C-3 position is replaced with primary or secondary amine or aminopyridine functionality. In particular, BMS-354326 (4) is a highly potent tryptase inhibitor (IC(50)=1.8 nM), which has excellent selectivity against trypsin and most Other related serine proteases.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z