anti-inflammatory agents

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

2-Amino-2-dichlorobenzophenone is an aromatic natural compound that has been used to study the effects of various compounds on cell metabolism, protein synthesis and enzyme activity. It has also been used in the synthesis of drugs, such as antitumor drugs and anti-inflammatory agents.

4-(3-chlorophenyl)-2,3-dihydro-1,3-thiazol-2-one has been used as a starting material for the synthesis of a variety of biologically active compounds, including antifungal, antiviral and anti-inflammatory agents.

1-(1-phenyltetrazol-5-yl)piperazine;hydrochloride (1-(1-phenyl-1H-1,2,3,4-tetrazol-5-yl)piperazine hydrochloride) is a chemical derivative of piperazine that has been used as a starting material for the synthesis of other compounds, such as anti-inflammatory agents. It modulates the activity of enzymes and proteins by binding to their active sites, and has been used in studies of enzyme inhibition and protein structure, as well as in drug metabolism.

Phthalide is a naturally occurring benzofuranone aromatic compound widely found in Apiaceae plants such as celery, angelica, and ligusticum. Phthalide can be used to synthesize various phthalate derivatives, including anti-inflammatory agents, antimicrobial agents, antioxidants, and blood-tumor barrier modulators.

Norketotifen is the active metabolite of Ketotifen. It exhibits anti-inflammatory activity on the skin, antimalarial properties, and non-histamine-mediated anti-itch effects in dogs. Norketotifen strongly inhibits the release of TNF-α without causing any sedative side effects and can be utilized in the study of non-sedative anti-inflammatory agents.

Isamfazone is utilized in the chemical and pharmacological studies on substituted pyridazones, the discovery of novel anti-inflammatory agents by aligning screening.

LY 269415 is an anti-inflammatory agent with antioxidant properties in vitro and could be beneficial as therapeutic agents in inflammatory arthritis.

Curdione ((+)-Curdione) inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be a candidate for anti-inflammatory and Y chemopreventive agents.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS/ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134

8-Epideoxyloganic acid possesses bioactivities of analgesia, homeostasis and anti-inflammatory. It has the potential to serve as anti-inflammatory agents during oxidative stress, the inhibition of ROS production, possibly through modulation of NOX activit

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate ((±)-Jasmonic Acid methyl ester) induces the synthesis of proteinase inhibitors in plant leaves, suppresses proliferation, and induces apoptosis in cancer cells. It inhibits hexokinase bound to mitochondria, disrupting mitochondrial hexokinase activity to selectively target and kill cancer cells. Derivatives of Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate also exhibit potential as anti-inflammatory agents, and the compound has been primarily detected in urine.

3-(2,6-dichlorophenyl)-1-methyl-7-(methylsulfanyl)-1H,2H,3H,4H-pyrimido[4,5-d][1,3]diazin-4-one is a compound that has been extensively investigated for the treatment of a variety of disorders including tumors, Alzheimer's and Parkinson's diseases, anti-inflammatory drugs, and analgesic agents.

WITHAFERIN A is a novel class of NFkappaB inhibitors, which hold promise as novel anti-inflammatory agents for treatment of various inflammatory disorders and/or cancer.

1. Acetylcorynoline (O-Acetylcorynoline) has antifungal,anti-inflammatory activity. 2. Acetylcorynoline may be one of the potent immunosuppressive agents through the blockage of dendritic cells maturation and function. 3. Acetylcorynoline is potential as a possible antiparkinsonian drug. (1) Significantly decreases dopaminergic neuron degeneration induced by 6-hydroxydopamine in BZ555 strain; (2) Prevents α-synuclein aggregation; (3) Restores food-sensing behavior, and dopamine levels; (4) Prolongs life-span in 6-hydroxydopamine-treated N2 strain. 4. Acetylcorynoline may exert its effects by decreasing egl-1 expression to suppress apoptosis pathways and by increasing rpn5 expression to enhance the activity of proteasomes.

1. Demethoxycurcumin (Desmethoxycurcumin) has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

INX-SM-6, a chemical compound, serves as a targeted delivery vehicle for anti-inflammatory agents and has shown efficacy in suppressing LPS-induced IL-1β production in human PBMCs [1].

Compound 8o (5-LOX/sEH-IN-1) is a dual inhibitor with cardioprotective properties, targeting both 5-LOX and sEH with IC50 values of 3.05 μM and 2.20 nM respectively. It also inhibits the activity of COX-2 (IC50=10.50 μM). Possessing analgesic and anti-inflammatory properties, 5-LOX/sEH-IN-1 reduces ulcerogenicity, making it a potential candidate for developing anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects.

Demethoxy Curcumin-D4 is a deuterated compound of Demethoxy Curcumin. Demethoxy Curcumin (T6S1683) has a CAS number of 22608-11-3. 1. Demethoxycurcumin has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.