In the last years, α1 adrenoceptors (α1-AR) have been the subject of intense research, in part because receptor-binding studies and molecular biology have opened up new aspects of understanding but also because of the potential to find new drugs possibly acting toward pathophysiological processes where α1-AR are involved, such as benign prostatic hyperplasia (BPH) or hypertension. At present, arylpiperazines represent one of the most studied classes of molecules with affinity at α1-AR. In fact, a large amount of work has been done and reported, describing synthetic procedures, biological evaluation at both α1-AR and the corresponding subtypes, and structure-activity relationships (SARs). In this paper, a review based on a literature survey aimed at focusing on the structural properties that a compound should possess to show affinity toward α1-AR is presented. Moreover, the identification and optimization of the structural features of a hit compound derived from a pharmacophore-based database search, leading to a new class of arylpiperazinylalkyl pyridazinone derivatives with α1-AR affinity is reported.

Manetti, F., Corelli, F., Strappaghetti, G., Botta, M. (2002). Arylpiperazines with high affinity toward a1-adrenergic receptors. CURRENT MEDICINAL CHEMISTRY, 9(13), 1303-1321.

Arylpiperazines with high affinity toward a1-adrenergic receptors

MANETTI, FABRIZIO;CORELLI, FEDERICO;BOTTA, MAURIZIO
2002-01-01

Abstract

In the last years, α1 adrenoceptors (α1-AR) have been the subject of intense research, in part because receptor-binding studies and molecular biology have opened up new aspects of understanding but also because of the potential to find new drugs possibly acting toward pathophysiological processes where α1-AR are involved, such as benign prostatic hyperplasia (BPH) or hypertension. At present, arylpiperazines represent one of the most studied classes of molecules with affinity at α1-AR. In fact, a large amount of work has been done and reported, describing synthetic procedures, biological evaluation at both α1-AR and the corresponding subtypes, and structure-activity relationships (SARs). In this paper, a review based on a literature survey aimed at focusing on the structural properties that a compound should possess to show affinity toward α1-AR is presented. Moreover, the identification and optimization of the structural features of a hit compound derived from a pharmacophore-based database search, leading to a new class of arylpiperazinylalkyl pyridazinone derivatives with α1-AR affinity is reported.
2002
Manetti, F., Corelli, F., Strappaghetti, G., Botta, M. (2002). Arylpiperazines with high affinity toward a1-adrenergic receptors. CURRENT MEDICINAL CHEMISTRY, 9(13), 1303-1321.
File in questo prodotto:
File Dimensione Formato  
2002CurrMedChemArylpiperazines.pdf

non disponibili

Tipologia: Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 363.02 kB
Formato Adobe PDF
363.02 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/22493
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo