Bioorganic & Medicinal Chemistry Letters 2009-07-01

Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.

Minoru Moriya, Hiroyuki Kishino, Shunji Sakuraba, Toshihiro Sakamoto, Takuya Suga, Hidekazu Takahashi, Takao Suzuki, Masahiko Ito, Junko Ito, Ryuichi Moriya, Norihiro Takenaga, Hisashi Iwaasa, Akane Ishihara, Akio Kanatani, Takehiro Fukami

Index: Bioorg. Med. Chem. Lett. 19(13) , 3568-72, (2009)

Full Text: HTML

Abstract

A series of 2-aminobenzimidazole-based MCH1R antagonists was identified by core replacement of the aminoquinoline lead 1. Subsequent modification of the 2- and 5-positions led to improvement in potency and intrinsic clearance. Compound 25 exhibited good plasma and brain exposure, and attenuated MCH induced food intake at 30mg/kg PO in rats.

Related Compounds

Related Articles:

Aggregation of 2-aminobenzimidazole--a combined experimental and theoretical investigation.

2011-06-20

[ChemPhysChem 12(9) , 1747-55, (2011)]

Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

2009-08-01

[Bioorg. Med. Chem. Lett. 19(15) , 4380-4, (2009)]

Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C.

2010-03-19

[ACS Chem. Biol. 5 , 287-299, (2010)]

Synthesis and QSAR studies of novel 1-substituted-2-aminobenzimidazoles derivatives.

2006-09-01

[Eur. J. Med. Chem. 41(9) , 1080-3, (2006)]

Experimental and theoretical (DFT) characterization of the excited states and N-centered radical species derived from 2-aminobenzimidazole, the core substructure of a family of bioactive compounds.

2010-05-20

[J. Phys. Chem. B 114(19) , 6608-13, (2010)]

More Articles...