Ontology highlight
ABSTRACT:
SUBMITTER: Liu W
PROVIDER: S-EPMC6231188 | biostudies-literature | 2018 Nov
REPOSITORIES: biostudies-literature
Liu Weiguo W Hussain Zahid Z Zang Yi Y Sweis Ramzi F RF Romero F Anthony FA Finke Paul E PE Moningka Remond R Bao Jianming J Plotkin Michael A MA Shang Jin J Dingley Karen H KH Salituro Gino G Murphy Beth Ann BA Howard Andrew D AD Ujjainwalla Feroze F Wood Harold B HB Duffy Joseph L JL
ACS medicinal chemistry letters 20181005 11
A series of structurally diverse azaspirodecanone and spirooxazolidinone analogues were designed and synthesized as potent and selective somatostatin receptor subtype 5 (SSTR5) antagonists. Four optimized compounds each representing a subseries showed improvement in their metabolic stability and pharmacokinetic profiles compared to those of the original lead compound <b>1</b> while maintaining pharmacodynamic efficacy. The optimized cyclopropyl analogue <b>13</b> demonstrated efficacy in a mouse ...[more]