MCH-R1 antagonists: what is keeping most research programs away from the clinic?
JL Méndez-Andino, JA Wos - Drug discovery today, 2007 - Elsevier
Despite the high number of drug-discovery programs dedicated to finding small-molecule
MCH-R1 antagonists for the treatment of obesity and/or mood disorders, a very limited …
MCH-R1 antagonists for the treatment of obesity and/or mood disorders, a very limited …
Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1, 3-(benzo) thiazol-2-yl]-ω-[3, 4 …
A Zablotskaya, I Segal, A Geronikaki… - European Journal of …, 2013 - Elsevier
A series of new N-[(benzo) thiazol-2-yl]-2/3-[3, 4-dihydroisoquinolin-2 (1H)-yl]
ethan/propanamide derivatives was synthesized and characterized by 1 H, 13 C NMR and …
ethan/propanamide derivatives was synthesized and characterized by 1 H, 13 C NMR and …
Discovery and development of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity
LL Rokosz - Expert Opinion on Drug Discovery, 2007 - Taylor & Francis
The melanin-concentrating hormone (MCH) is a hypothalamic peptide that binds to one of
two receptors: MCH1 and MCH2. MCH1 is well-recognized for its orexigenic properties but …
two receptors: MCH1 and MCH2. MCH1 is well-recognized for its orexigenic properties but …
Identification of Novel 1-O-Substituted Aporphine Analogues as Potent 5-HT2C Receptor Agonists
Q Mao, B Zhang, W Li, S Tian, W Shui… - ACS Chemical …, 2020 - ACS Publications
The 5-HT2C receptor has emerged as a promising target in the treatment of a variety of
central nervous system disorders. We have first identified aporphines as a new class of 5 …
central nervous system disorders. We have first identified aporphines as a new class of 5 …
Promising strategies for obesity pharmacotherapy: melanocortin-4 (MC-4) receptor agonists and melanin concentrating hormone (MCH) receptor-1 antagonists
MK Jeon, HG Cheon - Current topics in medicinal chemistry, 2009 - ingentaconnect.com
Despite remarkable progress in the elucidation of energy balance and regulation, the
development of new antiobesity drugs is still at the stage of infancy. Herein we briefly …
development of new antiobesity drugs is still at the stage of infancy. Herein we briefly …
Melanin-concentrating hormone receptor-1 antagonists as antiobesity therapeutics: current status
TJ Kowalski, T Sasikumar - BioDrugs, 2007 - Springer
There is compelling genetic and pharmacologic evidence to indicate that melanin-
concentrating hormone receptor-1 (MCHR1) signaling is involved in the regulation of food …
concentrating hormone receptor-1 (MCHR1) signaling is involved in the regulation of food …
Benzenesulfonamide compounds and the use thereof
A Matsumura, H Mikamiyama, B Shao, N Tsuno… - US Patent …, 2015 - Google Patents
4,145,427 A 3/1979 Langbein et al.(() p 5,028,519 A 7/1991 Morigaki et al. 5,688,960 A
11/1997 Shankar N 5,696,267 A 12/1997 Reichard et al. V 5,723,490 A 3/1998 Tung Z …
11/1997 Shankar N 5,696,267 A 12/1997 Reichard et al. V 5,723,490 A 3/1998 Tung Z …
Melanin concentrating hormone receptor antagonists as antiobesity agents: from M2 to MCHR-1
MD McBriar - Current Topics in Medicinal Chemistry, 2007 - ingentaconnect.com
Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS
of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 …
of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 …
Privileged heterocycles: bioactivity and synthesis of 1, 9-diazaspiro [5.5] undecane-containing compounds
D Blanco-Ania, R Heus, FPJT Rutjes - Chemistry of Heterocyclic …, 2017 - Springer
This review discusses the biological activity and synthesis of 1, 9-diazaspiro [5.5]
undecanes, including those ring-fused with arenes and heteroarenes and/or containing a …
undecanes, including those ring-fused with arenes and heteroarenes and/or containing a …
Benzenesulfonyl compounds and the use thereof
DJ Kyle, J Yao - US Patent 8,399,486, 2013 - Google Patents
The invention relates to pyrrolidinyl, piperidinyl, and hexahy droaZepinyl compounds of
Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, Wherein R1 …
Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, Wherein R1 …