Related Experiment Video
Updated: Aug 11, 2026
Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
The discovery of small molecule inhibitors of neutral endopeptidase. Structure-activity studies on functionalized
Graham N Maw1, Alan Stobie, Simon Planken
1Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
Abstract:
A series of small molecule glutaramides were synthesized and evaluated for potency against canine and human neutral endopeptidase using target criteria of molecular weight <400 and log P between 2 and 4.5 to maximize the likelihood of achieving good oral absorption. The structure-activity relationship (SAR) investigations described in this paper led to the identification of an ethyl 1,3,4-thiadiazole glutaramide which demonstrated good neutral endopeptidase potency, selectivity and excellent oral absorption in the rat.
