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image of Novel Compounds in Targeting the α1-adrenoceptor for Antihypertensive Therapy

Abstract

Hypertension, a prevalent cardiovascular condition, increases the risk of strokes and myocardial infarctions by inducing elevated blood pressure. Its prevalence has risen, particularly in low- and middle-income nations. The incidence of hypertension in adults is higher in low- and middle-income countries compared to high-income nations. One significant class of antihypertensive drugs is α1-adrenoceptor antagonists, which inhibit α1-adrenergic receptors and promote vasodilation. Terazosin, doxazosin, tamsulosin, and alfuzosin are examples of α1-adrenoceptor antagonists that have antihypertensive properties; however, they are linked to considerable side effects, including headaches, dizziness, reproductive problems, and postural hypotension. In the last several years, a number of novel α1-adrenergic antagonists have been synthesised by modifications of various pharmacophores such as Isochroman-4-one, Quinazolines, Piperazine, and Quinazoline-triazole, . The present review highlights recently synthesized α1-adrenoceptor antagonists for the management of hypertension, and emphasizes their structure-activity relationship and subtype selectivity.

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2025-10-03
2025-11-16

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Novel Compounds in Targeting the α1-adrenoceptor for Antihypertensive Therapy
Bentham Science Publishers ; https://doi.org/10.2174/0118715257395367250920224239
/content/journals/chamc/10.2174/0118715257395367250920224239
/content/journals/chamc/10.2174/0118715257395367250920224239
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  • Article Type:     Review Article
Keywords: subtype selectivity ; cardiovascular agents ; antihypertensive analogues ; α1-adrenoceptor antagonists ; structure-activity relationship (SAR) ; novel α1-adrenergic blockers

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