Synthesis and Structure–Activity Relationship of Naphtho[1,2-b]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists
スポンサーリンク
概要
- 論文の詳細を見る
The discovery that novel naphtho[1,2-b]furan-2-carboxamides containing linked piperidinylphenylacetamide groups serve as melanin concentrating hormone receptor 1 (MCH-R1) antagonists is described. An extensive structure–activity relationship (SAR) study, probing members of this family that contain a variety of aryl and heteroaryl groups at C-5 of the naphtho[1,2-b]furan-2-carboxamide skeleton and having different chain linker lengths, led to the identification of the 5-(4-pyridinyl) substituted analog 10b as a highly potent MCH-R1 antagonist with an IC50 value of 3 n<span style="font-variant: small-caps;">M</span>. This substance also displays good metabolic stability and it does not significantly inhibit cytochrome P450 (CYP450) enzymes. However, 10b has unacceptable oral bioavailability.
- 公益社団法人 日本薬学会の論文
著者
-
Lee Byung
Division Of Toxicology College Of Pharmacy Sungkyunkwan University
-
LIM Chae
Division of Applied Life Science (BK21 Program), and Plant Molecular Biology and Biotechnology Research Center, Gyeongsang National University
-
Choi Jun
Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul St. Mary's Hospital, The Catholic University of Korea
-
Oh Kwang-Seok
Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
-
Yi Kyu
Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
-
Lee Byung
Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
-
Choi Jun
Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
関連論文
- Evaluation of liver and thyroid toxicity in Sprague-Dawley rats after exposure to polybrominated diphenyl ether BDE-209
- Hypothyroidism protects di(n-butyl) phthalate-induced reproductive organs damage in Sprague-Dawley male rats
- Ras Transgene Expression in TG-AC Mice Treated with Benzo[a]pyrene
- POTENTIAL ESTROGENIC EFFECTS OF BISPHENOL : A ESTIMATED BY IN VITRO AND IN VIVO COMBINATION ASSAYS
- Association of Helicobacter pylori Infection with Gastric Adenocarcinoma
- 21C-10-1 Inducible nitric oxide synthase mRNA is upregulated in skin tumors of v-Ha-ras transgenic TG-AC mice treated with benzo(a)prene or 12-O-tetradecanoylphorbol-13-acetate.
- シロイヌナズナ懸濁培養細胞の高温順化過程での遺伝子発現プロフィール
- Effects of Di(2-ethylhexyl) Phthalate on Regulation of Steroidogenesis or Spermatogenesis in Testes of Sprague-Dawley Rats
- Pn-AMP1, a Plant Defense Protein, Induces Actin Depolarization in Yeasts
- Assessment of the phototoxic hazard of some chemicals using 3T3NRU assay and reconstructed human skin models
- Inducible Nitric Oxide Synthase mRNA Is Upregulated in Skin Tumors of v-Ha-ras Transgenic TG-AC Mice Treated with 12-o-Tetradecanoylphorbol-13-acetate
- O-11 Mechanistic role of benzo[a]pyrene in human stomach cancer(ACEM Oral Presentation III)
- Response to Letter to the Editor
- NDP kinase 2 regulates expression of antioxidant genes in Arabidopsis
- P159 Mechanistic role of benzo[a]pyrene in human stomach cancer
- E2-5 Effect of Nilotinib on Airway Remodeling in a Murine Model of Chronic Asthma(English Session 2)
- Synthesis and Structure–Activity Relationship of Naphtho[1,2-b]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists