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Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N1-agmatine and synthetic analogues (Articolo in rivista)

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Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N1-agmatine and synthetic analogues (Articolo in rivista) (literal)

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CARMIGNANI M.1, VOLPE A.R. 2, BOTTA B.3, ESPINAL R.4, DE BONNEVAUX S.C.5, DE LUCA C.6, BOTTA M.7, CORELLI F.8,TAFI A.9, SACCO R.10, DELLE MONACHE G.11.. (2001)
Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N1-agmatine and synthetic analogues
in Journal of medicinal chemistry
(literal)

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CARMIGNANI M.1, VOLPE A.R. 2, BOTTA B.3, ESPINAL R.4, DE BONNEVAUX S.C.5, DE LUCA C.6, BOTTA M.7, CORELLI F.8,TAFI A.9, SACCO R.10, DELLE MONACHE G.11.. (literal)

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Lavoro interdisciplinare (chimico/farmacologico) necessario al completamento dello studio relativo ai prodotti della Verbesina Caracasana e a prodotti da noi sintetizzati analoghi ai naturali. Studio che ha portato alla scoperta di prodotti sintetici più efficaci e migliori degli analoghi naturali. Questi prodotti seguono un brevetto internazionale di alcuni degli autori della pubblicazione, di proprietà del CNR e ne sono il naturale proseguimento, indispensabile per l'utilizzazione di alcune di queste sostanze come farmaci antiipertensivi. L'importanza del \"prodotto\" si evince dalla pubblicazione dello studio su J. Med. Chem. (fattore d'impatto = 4,566) e dal fatto che la stessa Rivista ha pubblicato, prima e dopo, diversi altri articoli correlati degli stessi autori. (literal)

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The more polar metabolites from the Venezuelan plant Verbesina caracasana, i.e., N3-prenylagmatine, (3,4-dimethoxycinnamoyl)-N1-agmatine, agmatine, and galegine (prenylguanidine), previously reported (Delle Monache, G.; et al. BioMed. Chem. Lett. 1999, 9, 3249-3254), have been synthesized following a biosynthetic strategy. The pharmacol. profiles of various synthetic analogs of (3,4-dimethoxycinnamoyl)-N1-agmatine (G5) were also analyzed, to shed some light on the structure-activity relationship of these compds. Derivs. with the (E)-configuration and/or with a p-methoxybenzoyl moiety were found to be responsible for higher hypotensive effects, which were assocd. with a slight and, in some cases, not dose-related increase of cardiac inotropism, with variable and not significant chronotropic responses, and, only at higher doses, with effects of respiratory depression. Either an increase (to six) or a decrease (to two) of the no. of methylene groups in the alkyl chain of (E)-G5 did not change blood pressure responses, while slightly increasing the pos. inotropic ones. At pharmacol. doses, all the studied compds. showed hypotensive and slight pos. inotropic effects without relevant chronotropic and respiratory actions. (literal)

Note

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1 Uni L'Aquila,2 CNR, 3 Uni Cattolica, 4 Uni Carabobo, 5 Uni Carabobo, 6 CNR, 7 Uni Siena, 8 Uni Siena,9 Uni Siena, 10 Uni Catanzaro, 11 CNR. (literal)

Titolo

Novel hypotensive agents from Verbesina caracasana. 8. Synthesis and pharmacology of (3,4-dimethoxycinnamoyl)-N1-agmatine and synthetic analogues (literal)

Abstract

The more polar metabolites from the Venezuelan plant Verbesina caracasana, i.e., N3-prenylagmatine, (3,4-dimethoxycinnamoyl)-N1-agmatine, agmatine, and galegine (prenylguanidine), previously reported (Delle Monache, G.; et al. BioMed. Chem. Lett. 1999, 9, 3249-3254), have been synthesized following a biosynthetic strategy. The pharmacol. profiles of various synthetic analogs of (3,4-dimethoxycinnamoyl)-N1-agmatine (G5) were also analyzed, to shed some light on the structure-activity relationship of these compds. Derivs. with the (E)-configuration and/or with a p-methoxybenzoyl moiety were found to be responsible for higher hypotensive effects, which were assocd. with a slight and, in some cases, not dose-related increase of cardiac inotropism, with variable and not significant chronotropic responses, and, only at higher doses, with effects of respiratory depression. Either an increase (to six) or a decrease (to two) of the no. of methylene groups in the alkyl chain of (E)-G5 did not change blood pressure responses, while slightly increasing the pos. inotropic ones. At pharmacol. doses, all the studied compds. showed hypotensive and slight pos. inotropic effects without relevant chronotropic and respiratory actions. (literal)

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