𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Azabicyclic indole esters as potent 5-HT4 receptor antagonists

✍ Scribed by Paul A. Wyman; Laramie M. Gaster; Frank D. King; Jonathon M. Sutton; Elizabeth S. Ellis; Kay A. Wardle; Timothy J. Young

Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
641 KB
Volume
4
Category
Article
ISSN
0968-0896

No coin nor oath required. For personal study only.

✦ Synopsis

The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon longitudinal muscle myenteric plexus preparation.

πŸ“œ SIMILAR VOLUMES

ChemInform Abstract: Substituted Indole-
ChemInform Abstract: Substituted Indole-5-carboxamides and -acetamides as Potent Nonpeptide GnRH Receptor Antagonists.
✍ Wallace T. Ashton; Rosemary M. Sisco; Yi Tien Yang; Jane-Ling Lo; Joel B. Yudkov πŸ“‚ Article πŸ“… 2010 πŸ› John Wiley and Sons βš– 29 KB πŸ‘ 1 views

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a β€œFull Text” option. The original article is trackable v

Synthesis and pharmacological evaluation
Synthesis and pharmacological evaluation of aryl aminosulfonamide derivatives as potent 5-HT6 receptor antagonists
✍ Ramakrishna V.S. Nirogi; Anand V. Daulatabad; G. Parandhama; Shaikh Mohammad; K. πŸ“‚ Article πŸ“… 2010 πŸ› Elsevier Science 🌐 English βš– 410 KB

A series of novel aryl aminosulfonamides was designed and synthesized as 5-HT 6 receptor ligands. Many compounds screened in a functional reporter gene based assay displayed potent antagonistic activity with Kb values in the range of 0.02-10 nM. The lead compound 11m exemplified in this series showe