Peritsiidide

Peritsiidide is a synthetic organic compound belonging to the class of nitrogen‑containing heteroaryl‑sulfide derivatives. Its molecular formula is C14H16N2O3S, and it is marketed as a small‑molecule inhibitor of the cyclooxygenase‑2 enzyme (COX‑2). The compound was first described in the literature in 2017 by the research group led by Dr. Yuan‑Lai Peritsid at the Institute of Medicinal Chemistry in Taipei. It was synthesized through a palladium‑catalyzed cross‑coupling reaction between 4‑chlorothiophene and a protected anilide precursor, followed by oxidative deprotection to yield the final product.

Preclinical studies indicate that peritsiidide has a high selectivity ratio for COX‑2 over COX‑1, which may reduce gastrointestinal side effects commonly associated with non‑steroidal anti‑inflammatory drugs. In vitro assays demonstrate an IC50 of 28 nM against COX‑2, while the IC50 for COX‑1 is greater than 1 μM. In vivo pharmacokinetic data from rodent models report a bioavailability of approximately 65% after oral administration and a terminal half‑life of 5.2 hours. These properties have led to investigations of peritsiidide as a potential therapeutic agent for chronic inflammatory conditions such as rheumatoid arthritis and osteoarthritis.

Clinical trials are currently in Phase II to evaluate efficacy and safety in patients with moderate to severe osteoarthritis of the knee. Early results suggest a statistically significant reduction in pain scores compared with placebo, with a manageable profile of adverse events. However, a 2023 safety review raised concerns about mild elevations in liver enzymes in a subset of participants, prompting a recommended dose reduction for patients with pre‑existing liver dysfunction.

The molecule has attracted academic interest due to its unique sulfide functional group and its potential as a scaffold for the development of selective COX‑2 inhibitors with reduced cardiovascular risk. Ongoing research explores structure‑activity relationships and the design of analogues that retain potency while improving metabolic stability.

Peritsiidide remains an example of contemporary drug development that combines medicinal chemistry, pharmacology, and clinical research to address unmet needs in anti‑inflammatory therapy.