Arylpiperazines with Affinity Toward a1-Adrenergic Receptors

Authors: Manetti F.; Corelli F.; Strappaghetti G.; Botta M.

Source: Current Medicinal Chemistry, Volume 9, Number 13, July 2002 , pp. 1303-1321(19)

Publisher: Bentham Science Publishers

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Abstract:

In the last years, agr 1 adrenoceptors ( agr 1-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 agr 1-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 agr 1-AR. In fact, a large amount of work has been done and reported, describing synthetic procedures, biological evaluation at both agr 1-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 agr 1-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 agr 1-AR affinity is reported.

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

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/0929867023369961

Publication date: 2002-07-01

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Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.