Exploiting the 2-(1,3,4,9-tetrahydropyrano[3,4-<i>b</i>]indol-1-yl)acetic Acid Scaffold to Generate COXTRANs: A New Class of Dual Cyclooxygenase Inhibitors-Thromboxane Receptor Antagonists.

ABSTRACT: The use of traditional nonsteroidal anti-inflammatory drugs (NSAIDs) and coxibs is effective for the treatment of inflammatory pain and chronic inflammatory conditions. However, their use is associated with enhanced risk of cardiovascular toxicity and thrombotic events, particularly for the latter. The vascular side effects of these drugs could be mitigated by pharmacological inhibition of the thromboxane A₂ receptor (TP). Here we describe the development of a new class of dual cyclooxygenase (COX) inhibitors/thromboxane receptor antagonists (COXTRANs) based on the 2-(1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl)acetic acid scaffold. The in vitro evaluation of 50 newly synthesized compounds resulted in a set of well-balanced compounds exhibiting nanomolar activity on both CO

SUBMITTER: Blua F 

PROVIDER: S-EPMC12621201 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature