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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Arylpiperazines with Affinity Toward a1-Adrenergic Receptors

Author(s): F. Manetti, F. Corelli, G. Strappaghetti and M. Botta

Volume 9 , Issue 13 , 2002

Page: [1303 - 1321] Pages: 19

DOI: 10.2174/0929867023369961

Price: $65


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.

Keywords: arylpiperazine, 1-adrenergic receptor, alpha1-ar, pyridazinone derivative

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