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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. DOI: 10.5935/1984-6835.20130084A obesidade é uma doença crônica que é caracterizada por um acúmulo de excesso de tecido adiposo. Atualmente, existem alguns medicamentos seguros e eficazes para o tratamento farmacológico da obesidade. Portanto, torna-se necessário o desenvolvimento de novas drogas. Na última década, o alvo mais promissor para a obesidade foi o hormônio concentrador de melanina. Com isso, diversas indústrias farmacêuticas desenvolveram peptídeos e pequenas moléculas como antagonistas MCH-R1, mas estes compostos apresentaram problemas como afinidade para o canal hERG e perfil farmacocinético pobre. Neste artigo, fizemos uma breve revisão da concepção da estratégia mais relevante e relações da estrutura-atividade no desenvolvimento de carboxamida, ureias, quinolina e derivados quinazolina como antagonistas MCH-R1. DOI: 10.5935/1984-6835.2013008

MCH-R1 Antagonists as Potential Anti-obesity Drugs. Design Strategies and Structure-activity Relationship