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Titolo:
SYNTHESIS AND ALPHA(2)-ADRENERGIC ACTIVITY OF 2-[(METHYLENEAMINO)OXY]-N-(GUANIDINO)ETHANEIMINES - A BIOISOSTERIC REPLACEMENT OF THE ARYL OFGUANABENZ-TYPE BENZYLIDENEAMINOGUANIDINE ALPHA(2)-AGONISTS WITH THE [(METHYLENEAMINO)OXY]METHYL MOIETY (MAOMM)
Autore:
BALSAMO A; GENTILI D; MACCHIA M; MARTINOTTI E; ROSSELLO A; SCATIZZI R;
Indirizzi:
UNIV PISA,DIPARTIMENTO SCI FARMACEUT,VIA BONANNO 6 I-56100 PISA ITALY UNIV PISA,IST POLICATTEDRA DISCIPLINE BIOL I-56100 PISA ITALY
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 9, volume: 31, anno: 1996,
pagine: 713 - 716
SICI:
0223-5234(1996)31:9<713:SAAAO2>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTIINFLAMMATORY ACTIVITY; DESIGN; SERIES; ACIDS;
Keywords:
ALPHA(2)-ADRENERGIC AGONIST; AMINOGUANIDINE ADRENERGIC DRUG; GUANABENZ ANALOG; 2-[(METHYLENEAMINO)OXY]-N-(GUANIDINO)ETHANE-IMINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
16
Recensione:
Indirizzi per estratti:
Citazione:
A. Balsamo et al., "SYNTHESIS AND ALPHA(2)-ADRENERGIC ACTIVITY OF 2-[(METHYLENEAMINO)OXY]-N-(GUANIDINO)ETHANEIMINES - A BIOISOSTERIC REPLACEMENT OF THE ARYL OFGUANABENZ-TYPE BENZYLIDENEAMINOGUANIDINE ALPHA(2)-AGONISTS WITH THE [(METHYLENEAMINO)OXY]METHYL MOIETY (MAOMM)", European journal of medicinal chemistry, 31(9), 1996, pp. 713-716

Abstract

Some 2-[(methyleneamino)oxy]-N-(guanidino)ethaneimines (10a-g) were synthesized as analogs of guanabenz-type benzylideneaminoguanidine alpha(2)-agonists (9) in which the aryl portion (Ar) is substituted by the[(methyleneamino)oxy]methyl moiety (MAOMM). The alpha(2)-adrenergic activity of compounds 10a-g was evaluated by functional tests on guinea-pig ileum. The MAOM-derivatives 10a-g exhibited an alpha(2)-adrenergic stimulating activity fairly similar to that of the benzylideneaminoguanidine reference drug guanabenz, thus supporting the hypothesis of the existence of a bioisoster-like relationship between the MAOMM and the Ar in the class of guanabenz-type alpha(2)-adrenergic agonists.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 06:44:16