TY - JOUR
T1 - MCH-R1 antagonists as potential anti-obesity drugs. Design strategies and structure-activity relationship
AU - Rivera, Gildardo
AU - Moreno, Antonio
AU - Bocanegra-García, Virgilio
PY - 2013
Y1 - 2013
N2 - Obesity is a chronic disease that is characterized by an accumulation of excess adipose tissue. Actually, there are few safe and effective drugs for pharmacological treatment of obesity. Therefore, it becomes necessary the development of new drugs. In the last decade, the most promising target for obesity was melanin-concentrating hormone. Thereat, diverse pharmaceutical companies developed peptides and small molecules as MCH-R1 antagonists, but, these compounds had problems as affinity for hERG channel and poor pharmacokinetic profile. In this manuscript, we made a brief review of the most relevant strategy design and structure-activity relationships in the development of carboxamide, ureas, quinoline, and quinazoline derivatives as MCH-R1 antagonists.
AB - Obesity is a chronic disease that is characterized by an accumulation of excess adipose tissue. Actually, there are few safe and effective drugs for pharmacological treatment of obesity. Therefore, it becomes necessary the development of new drugs. In the last decade, the most promising target for obesity was melanin-concentrating hormone. Thereat, diverse pharmaceutical companies developed peptides and small molecules as MCH-R1 antagonists, but, these compounds had problems as affinity for hERG channel and poor pharmacokinetic profile. In this manuscript, we made a brief review of the most relevant strategy design and structure-activity relationships in the development of carboxamide, ureas, quinoline, and quinazoline derivatives as MCH-R1 antagonists.
KW - Antagonists
KW - Melanin-concentrating hormone
KW - Obesity
UR - http://www.scopus.com/inward/record.url?scp=84891406483&partnerID=8YFLogxK
U2 - 10.5935/1984-6835.20130084
DO - 10.5935/1984-6835.20130084
M3 - Artículo
SN - 1984-6835
VL - 5
SP - 1156
EP - 1178
JO - Revista Virtual de Quimica
JF - Revista Virtual de Quimica
IS - 6
ER -