Evolution of physicochemical properties of melanin concentrating hormone receptor 1 (MCHr1) antagonists

A Johansson - Bioorganic & Medicinal Chemistry Letters, 2016 - Elsevier
Bioorganic & Medicinal Chemistry Letters, 2016Elsevier
One pharmacological principle for the treatment of obesity is blockade of the melanin
concentrating hormone receptor 1 (MCHr1), which in rodents has been shown to be strongly
associated with food intake and energy expenditure. However, discovery of safe and
efficacious MCHr1 antagonists has proved to be complex. So far, six compounds have been
progressed into clinical trials, but clinical validation of the concept is still lacking. An account
of discovery of the three most recent clinical candidates targeting the MCHr1 receptor is …
Abstract
One pharmacological principle for the treatment of obesity is blockade of the melanin concentrating hormone receptor 1 (MCHr1), which in rodents has been shown to be strongly associated with food intake and energy expenditure. However, discovery of safe and efficacious MCHr1 antagonists has proved to be complex. So far, six compounds have been progressed into clinical trials, but clinical validation of the concept is still lacking. An account of discovery of the three most recent clinical candidates targeting the MCHr1 receptor is given, with an emphasis on their physicochemical properties.
Elsevier