cox-1

COX-1/2-IN-3 (Compound 7a) is a dual inhibitor of COX-1 and COX-2, exhibiting anti-inflammatory activity with low toxicity [1].

COX-1/2-IN-2, a potent inhibitor of both COX-1 and COX-2, demonstrates significant inhibitory activity, with IC50 values of 13.9 ± 3.21 μM for COX-1 and 6.4 ± 0.74 μM for COX-2, respectively [1].

COX-1/2-IN-2 is a potent inhibitor of both COX-1 and COX-2, with IC50 values of 9.7 ± 0.09 μM for COX-1 and 4.6 ± 1.45 μM for COX-2, respectively [1].

COX-1/2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2, and demonstrates moderate anticancer activity with IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].

COX-1/2-IN-5 (compound 2a) is a dual inhibitor of COX1/2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity against liver cancer HepG2 cells with an IC50 of 60.75 μM [1].

COX-1/2-IN-6 (compound 4 h) acts as a dual inhibitor of COX-1 and COX-2, exhibiting potent inhibitory activity with IC50 values of 68 nM and 91 nM, respectively. It is utilized in the research of inflammatory diseases [1].

COX-1/2-IN-8 (compound 11f) is an orally active inhibitor of both COX-1 and COX-2, with IC50 values of 2.14 µM and 0.58 µM, respectively. Its anti-inflammatory activity surpasses that of celecoxib.

COX-1/2-IN-9 (Compound 3n) serves as a selective and potent inhibitor of both COX-1 and COX-2, demonstrating IC 50 values of 0.031 µM for COX-1 and 0.01 µM for COX-2. This compound exhibits antibacterial and anti-inflammatory properties, effectively targeting MRSA 1478 (MIC=50 μg/mL) and multidrug-resistant S. lentus (MIC=50 μg/mL). Furthermore, COX-1/2-IN-9 shows promise in relieving MRSA-induced pneumonia in conditions of compromised immunity.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

(S)-Ketorolac is a potent inhibitor of COX1 and COX2 enzyme, and is nonsteroidal anti-inflammatory agent.

COX-1-IN-2 (compound 5h) serves as a potent anti-inflammatory and analgesic agent. This compound demonstrates a significant inhibitory effect on COX-1, with an IC 50 value of 38.76 nM.

COX-1-IN-1 (compound 15a) selectively inhibits cyclooxygenase (COX), exhibiting an IC50 of 0.23 μM for COX-1 and greater than 50 μM for COX-2, resulting in a selectivity index (COX-2 IC50/COX-1 IC50) of 217. Additionally, COX-1-IN-1 effectively inhibits platelet aggregation [1].

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities and inhibits Abeta (25 - 35) and Abeta (1 - 40) induced cell death.

Tenidap (CP-66248) is a selective COX-1 and SLC26A3 inhibitor with anti-inflammatory, analgesic, and anti-rheumatic activities.

BN-82451 2HCl is a dual inhibitor of COX-1 and COX-2 and can be used to study Huntington's chorea and Parkinson's disease.

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

Vedaprofen (PM 150) inhibits COX-1 and reduces prostaglandin H2 synthesis with anti-inflammatory activities. Vedaprofen is an inhibitor of Escherichia coli sliding clamp with the IC50 of 222 μM and Ki of 131 μM.

Salicylamide (2-Hydroxybenzamide) is an over-the-counter drug with analgesic and antipyretic properties, which has similar medicinal properties to aspirin. In the over-the-counter pain remedies, Salicylamide is used in combination with both aspirin and caffeine.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Fenoprofen calcium is a propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.