Design, parallel synthesis and SAR of novel urotensin II receptor agonists

Lehmann, Fredrik, 1976 (author): Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry

Lake, Lisa (author)

Currier, Erika A. (author)

Olsson, Roger, 1967 (author): Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry

Hacksell, Uli (author)

Luthman, Kristina, 1953 (author): Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry

(creator_code:org_t)

Elsevier BV, 2007
2007
English.
In: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 42, s. 276-285

Related links:: https://gup.ub.gu.se...; show more...; https://doi.org/10.1...; show less...

Abstract Subject headings

A 30-membered library of amides based on the potent urotensin II (UII) receptor agonist FL104, has been synthesized from ten different carboxylic acids and three amines. A synthetic protocol producing the amides in 47-98% yield has been developed in which the purification involved only extractions and in a few cases filtration through an ion-exchange resin. It was found that 5 mg of starting material was enough to obtain reproducible results and excellent purities. Thus, the procedure is estimated to be transferable to fully automated systems. The synthesized compounds were evaluated for their UII receptor agonistic activities using a cell-based assay (R-SAT). The most active compounds were the 4-trifluoromethylcinnamic amides of 1-(4-chlorophenyl)-3-dimethylamino-propylamine and 1-(2-naphthyl)-3-dimethylamino-propylamine, both showed EC50 values of 130 nM. © 2006 Elsevier Masson SAS. All rights reserved.

MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)

By the author/editor: Lehmann, Fredrik ...; Lake, Lisa; Currier, Erika A ...; Olsson, Roger, 1 ...; Hacksell, Uli; Luthman, Kristin ...

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Medicinal Chemis ...

NATURAL SCIENCES: NATURAL SCIENCES; and Chemical Science ...; and Organic Chemistr ...

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Pharmacology and ...

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