188862-35-3Relevant academic research and scientific papers
Development of strategies for the site-specific in vivo incorporation of photoreactive amino acids: p-Azidophenylalanine, p-acetylphenylalanine and benzofuranylalanine
Behrens, Carsten,Nielsen, Jens N.,Fan, Xue-Jun,Doisy, Xavier,Kim, Ki-Hyun,Praetorius-Ibba, Mette,Nielsen, Peter E.,Ibba, Michael
, p. 9443 - 9449 (2000)
A major limitation of conventional site-directed mutagenesis is that substitutions are restricted to the 20 naturally occurring amino acids. While this problem can be circumvented in vitro to allow the site-specific incorporation of non-canonical amino acids, no similar in vivo methodologies yet exist. The main requirement for such a system is an aminoacyl-tRNA synthetase able to exclusively recognize a non-canonical amino acid and a suppressor tRNA. The engineering of such activities in aminoacyl-tRNA synthetases has proven to be problematic due to their high substrate specificity. Here we report progress towards the development of an antibody-based methodology to screen large mutant aminoacyl-tRNA synthetase libraries for specific recognition of the non-canonical photoreactive benzofuran amino acid [3-(5'-benzofuranyl)-alanine]. We also report the chemical synthesis and enantiomeric resolution of this amino acid. (C) 2000 Elsevier Science Ltd.
THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
-
, (2019/02/13)
Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
The discovery and preparation of disubstituted novel amino-aryl-piperidine- based renin inhibitors
Cody, Wayne L.,Holsworth, Daniel D.,Powell, Noel A.,Jalaie, Mehran,Zhang, Erli,Wang, Wei,Samas, Brian,Bryant, John,Ostroski, Robert,Ryan, Michael J.,Edmunds, Jeremy J.
, p. 59 - 68 (2007/10/03)
Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture of enantiomers that are potent in vitro renin inhibitors and also, possess in vivo antihypertensive activity in a double transgenic mouse model.
Piperidine derivative rennin inhibitors
-
Page/Page column 18, (2010/02/08)
Disclosed are piperidine derivatives, their manufacture and use as inhibitors of renin.
Piperidine derivatives having renin inhibiting activity
-
, (2008/06/13)
Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
