Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
Summary of "Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands."
Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT(1) and MT(2) receptors are reported. Compounds 11f and 18b (MT(1)/MT(2) agonist) have human microsomal intrinsic clearance comparable to ramelteon.
Affiliation
Department of Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Rd., Paramus, NJ 07652, USA.
Journal Details
This article was published in the following journal.
Name: Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Pages: 1236-42
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21237644
- DOI: http://dx.doi.org/10.1016/j.bmcl.2010.12.068
Medical and Biotech [MESH] Definitions
Phosphoribosylaminoimidazolecarboxamide Formyltransferase
An enzyme that catalyzes the conversion of aminoimidazole-4-carboxamide ribonucleotide to 5-formyl-aminoimidazole-4-carboxamide ribonucleotide in the purine de novo synthesis pathway. It requires the cofactor N(10)-FORMYLTETRAHYDROFOLATE as the formyl donor.
Cycloparaffins
Alicyclic hydrocarbons in which three or more of the carbon atoms in each molecule are united in a ring structure and each of the ring carbon atoms is joined to two hydrogen atoms or alkyl groups. The simplest members are cyclopropane (C3H6), cyclobutane (C4H8), cyclohexane (C6H12), and derivatives of these such as methylcyclohexane (C6H11CH3). (From Sax, et al., Hawley's Condensed Chemical Dictionary, 11th ed)
Amide Synthases
Enzymes that catalyze the joining of either ammonia or an amide with another molecule, in which the linkage is in the form of a carbon-nitrogen bond. EC 6.3.1.
Angiotensin Amide
The octapeptide amide of bovine angiotensin II used to increase blood pressure by vasoconstriction.
Synthetic Biology
A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.
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