Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs

José L. Falcó; Maia Lloveras; Irma Buira; Jordi Teixidó; José I. Borrell; Eva Méndez; José Terencio; Albert Palomer; Antonio Guglietta

doi:10.1016/j.ejmech.2005.06.008

Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs

José L. Falcó, Maia Lloveras, Irma Buira, Jordi Teixidó, José I. Borrell, Eva Méndez, José Terencio, Albert Palomer, Antonio Guglietta

IQS School of Engineering

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Among the known non-benzodiazepinic hypnotic drugs acting on the α1 subunit of the GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity and selectivity. Following a design methodology including pharmacophoric requirements and ADME-predicted properties, we have synthesized a library of 3-amino-4,5-dihydro-1H-pyrazolo[3,4-b]pyridin-6(7H)- ones (3) and their N1-alkyl derivatives (4) as new scaffolds for designing non-benzodiazepine BZ receptor ligands.

Idioma original	Anglès
Pàgines (de-a)	1179-1187
Nombre de pàgines	9
Revista	European Journal of Medicinal Chemistry
Volum	40
Número	11
DOIs	https://doi.org/10.1016/j.ejmech.2005.06.008
Estat de la publicació	Publicada - de nov. 2005

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10.1016/j.ejmech.2005.06.008

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Falcó, J. L., Lloveras, M., Buira, I., Teixidó, J., Borrell, J. I., Méndez, E., Terencio, J., Palomer, A., & Guglietta, A. (2005). Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs. European Journal of Medicinal Chemistry, 40(11), 1179-1187. https://doi.org/10.1016/j.ejmech.2005.06.008

@article{f3e3fde5cbbf4a2b955e20949dc42513,

title = "Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs",

abstract = "Among the known non-benzodiazepinic hypnotic drugs acting on the α1 subunit of the GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity and selectivity. Following a design methodology including pharmacophoric requirements and ADME-predicted properties, we have synthesized a library of 3-amino-4,5-dihydro-1H-pyrazolo[3,4-b]pyridin-6(7H)- ones (3) and their N1-alkyl derivatives (4) as new scaffolds for designing non-benzodiazepine BZ receptor ligands.",

keywords = "ADME, Catalyst, Combinatorial chemistry, GABA-A receptor, Indiplon, Non-benzodiazepinic, Pyrazolo[3,4-b]pyridin-6-ones, Volsurf, Zaleplon, Zolpidem",

author = "Falc{\'o}, {Jos{\'e} L.} and Maia Lloveras and Irma Buira and Jordi Teixid{\'o} and Borrell, {Jos{\'e} I.} and Eva M{\'e}ndez and Jos{\'e} Terencio and Albert Palomer and Antonio Guglietta",

year = "2005",

month = nov,

doi = "10.1016/j.ejmech.2005.06.008",

language = "English",

volume = "40",

pages = "1179--1187",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "11",

}

Falcó, JL, Lloveras, M, Buira, I, Teixidó, J , Borrell, JI, Méndez, E, Terencio, J, Palomer, A & Guglietta, A 2005, 'Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs', European Journal of Medicinal Chemistry, vol. 40, núm. 11, pàg. 1179-1187. https://doi.org/10.1016/j.ejmech.2005.06.008

Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs. / Falcó, José L.; Lloveras, Maia; Buira, Irma et al.
In: European Journal of Medicinal Chemistry, Vol. 40, Núm. 11, 11.2005, pàg. 1179-1187.

Producció científica: Article en revista indexada › Article › Avaluat per experts

TY - JOUR

T1 - Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs

AU - Falcó, José L.

AU - Lloveras, Maia

AU - Buira, Irma

AU - Teixidó, Jordi

AU - Borrell, José I.

AU - Méndez, Eva

AU - Terencio, José

AU - Palomer, Albert

AU - Guglietta, Antonio

PY - 2005/11

Y1 - 2005/11

N2 - Among the known non-benzodiazepinic hypnotic drugs acting on the α1 subunit of the GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity and selectivity. Following a design methodology including pharmacophoric requirements and ADME-predicted properties, we have synthesized a library of 3-amino-4,5-dihydro-1H-pyrazolo[3,4-b]pyridin-6(7H)- ones (3) and their N1-alkyl derivatives (4) as new scaffolds for designing non-benzodiazepine BZ receptor ligands.

AB - Among the known non-benzodiazepinic hypnotic drugs acting on the α1 subunit of the GABA-A receptor, Zolpidem (2a), Zaleplon (1b) and Indiplon (1a) have showed high affinity and selectivity. Following a design methodology including pharmacophoric requirements and ADME-predicted properties, we have synthesized a library of 3-amino-4,5-dihydro-1H-pyrazolo[3,4-b]pyridin-6(7H)- ones (3) and their N1-alkyl derivatives (4) as new scaffolds for designing non-benzodiazepine BZ receptor ligands.

KW - ADME

KW - Catalyst

KW - Combinatorial chemistry

KW - GABA-A receptor

KW - Indiplon

KW - Non-benzodiazepinic

KW - Pyrazolo[3,4-b]pyridin-6-ones

KW - Volsurf

KW - Zaleplon

KW - Zolpidem

UR - http://www.scopus.com/inward/record.url?scp=26844510933&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2005.06.008

DO - 10.1016/j.ejmech.2005.06.008

M3 - Article

C2 - 16095764

AN - SCOPUS:26844510933

SN - 0223-5234

VL - 40

SP - 1179

EP - 1187

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11

ER -

Design, synthesis and biological activity of acyl substituted 3-amino-5-methyl-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-ones as potential hypnotic drugs

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