Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated anal
Judd, Andrew S.,Souers, Andrew J.,Wodka, Dariusz,Zhao, Gang,Mulhern, Mathew M.,Iyengar, Rajesh R.,Gao, Ju,Lynch, John K.,Freeman, Jennifer C.,Falls, H. Douglas,Brodjian, Sevan,Dayton, Brian D.,Reilly, Regina M.,Gintant, Gary,Limberis, James T.,Mikhail, Ann,Leitza, Sandra T.,Houseman, Kathryn A.,Diaz, Gilbert,Bush, Eugene N.,Shapiro, Robin,Knourek-Segel, Victoria,Hernandez, Lisa E.,Marsh, Kennan C.,Sham, Hing L.,Collins, Christine A.,Kym, Philip R.
p. 2365 - 2371
(2008/02/01)
A novel and efficient route to zafirlukast
Zafirlukast, an important drug for allergic pulmonary disorders such as asthma, is synthesized by a five-step, high-yielding, and inexpensive process.