NPY 5RA972 - CAS 439861-56-0
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Neuropeptide Y receptor
NPY5RA972 is a neuropeptide Y Y5 antagonist.
≥98% by HPLC
NPY5RA972; NPY-5-RA-972; NPY 5 RA 972; N-[4-Methyl-9-(1-methylethyl)-9H-carbazol-3-yl]-4-morpholinecarboxamide
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1.Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity.
Block MH;Boyer S;Brailsford W;Brittain DR;Carroll D;Chapman S;Clarke DS;Donald CS;Foote KM;Godfrey L;Ladner A;Marsham PR;Masters DJ;Mee CD;O'Donovan MR;Pease JE;Pickup AG;Rayner JW;Roberts A;Schofield P;Suleman A;Turnbull AV J Med Chem. 2002 Aug 1;45(16):3509-23.
The hypothesis that antagonists of the neuropeptide Y5 receptor would provide safe and effective appetite suppressants for the treatment of obesity has prompted vigorous research to identify suitable compounds. We discovered a series of acylated aminocarbazole derivatives (e.g., 3a) that are potent and selective Y5 antagonists, representing interesting starting points but suffering from poor bioavailability and concerns about potential toxicity as a consequence of the embedded aminocarbazole fragment. It proved relatively easy to improve the drug metabolism and pharmacokinetic (DMPK) properties by variation of the side chain (as in 4a) but difficult to eliminate the aminocarbazole fragment. For compounds in this series to have the potential to be drugs, we believed that both the compound itself and the component aniline must be free of mutagenic activity. Parallel structure-activity relationship studies looking at the effects of ring substitution have proved that it is possible by incorporation of a 4-methyl substituent to produce carbazole ureas with potent Y5 activity, comprised of carbazole anilines that in themselves are devoid of mutagenic activity in the Ames test. Compound 4o (also known as NPY5RA-972) is highly selective with respect to Y1, Y2, and Y4 receptors (and also to a diverse range of unrelated receptors and enzymes), with an excellent DMPK profile including central nervous system penetration.
2.Efficient synthesis of ureas by direct palladium-catalyzed oxidative carbonylation of amines.
Gabriele B;Salerno G;Mancuso R;Costa M J Org Chem. 2004 Jul 9;69(14):4741-50.
A general synthesis of symmetrically disubstituted ureas and trisubstituted ureas by direct Pd-catalyzed oxidative carbonylation of primary amines or of a mixture of a primary and a secondary amine, respectively, with unprecedented catalytic efficiencies for this kind of process, is reported. Reactions are carried out at 90-100 degrees C in DME as the solvent in the presence of PdI(2) in conjunction with an excess of KI as the catalytic system and under 20 atm of a 4:1 mixture of CO and air. In some cases, working in the presence of an excess of CO(2) (40 atm) in addition to CO and air (60 atm total) had a beneficial effect on substrate reactivity and product yield. Cyclic five-membered and six-membered ureas were easily formed from primary diamines. The methodology has been successfully applied to the synthesis of pharmacologically active ureas, such as those deriving from alpha-amino esters or urea NPY5RA-972, a potent antagonist of the neuropeptide Y5 receptor.
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CAS 439861-56-0 NPY 5RA972

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