Aspirin (1) is a representative non-steroidal anti-inflammatory drug (nsaid) used as an analgesic, antipyretic, anti-inflammatory, and antiplatelet drug. The aim of this work was to design, synthesize and characterize the potential anti-nociceptive and anti-inflammatory activities of a new series of bioisosteres and hybrids from known non-steroidal anti-inflammatory drugs (nsaids. A mixture-based combinatorial library of five ugi adducts (4-8) incorporating known antitubercular and antimalarial pharmacophores was successfully synthesized, starting from the naturally occurring diisocyanide 3, via parallel ugi four-center three-component reactions (u-4c-3cr.
Colorectal cancer (crc) is a leading cause of death, providing impetus for discovery of new chemopreventive agents chemoprevention strategies for crc have targeted antiproliferative and anti-inflammatory actions on colonocytes containing populations subject to carcinogen-induced dna damage. Hybrid curcumin compounds: a new strategy for cancer treatment medicines as a potent anti-inflammatory agent connect two pharmacophores can vary and allow. Thus, anti-inflammatory drugs have been widely explored as chemopreventive and antineoplastic agents aspirin (asa), in particular, is associated with reduced breast cancer incidence but gastrointestinal toxicity has limited its usefulness.
Ty - jour t1 - spiroindoles as potential pharmacophores au - panda,siva s py - 2016/6/24 y1 - 2016/6/24 n2 - the spiroindole heterocyclic scaffold is found in many natural products and has been identified as an important bioactive agent. By using the multi-target-directed drug designing strategy, a highly promising anti-inflammatory agent capable to inhibit cyclooxygenase-2 (cox-2) and lipoxygenase (5-lox) enzymes of arachidonic acid metabolic pathway is developed. Introduction leukotriene a 4 hydrolase (lta 4h) is a metalloenzyme with both epoxide hydrolase and aminopeptidase activity the epoxide hydrolase activity of the enzyme converts. Introduction the advancement of novel chemotherapeutic agent is an imperative and demanding task for the medicinal chemist many research programs are aimed towards design and synthesis of new drugs. Non-steroidal anti-inflammatory drugs (nsaids) are one of the most widely prescribed drug categories against various inflammation mediated diseases, such as arthritis, rheumatism as well as to relieve the aches and pain of daily life 1-8 inflammation is the non-specific protective mechanistic action of the immune system, local biological.
Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents european journal of medicinal chemistry 46: 5763-5768. The anti-inflammatory and antiproliferative actions of gt-094 in vivo were recapitulated in vitro, and gt- 094 was seen to induce phase 2 enzymes via the antioxidant. New hybrid drugs are described with antioxidants built into anti-inflammatory pharmacophores hybrid drug efficacy can be greater than the individual components used at the same concentration hybrid antioxidant drugs show efficacy for non-responsive lung cancers linked to inflammation.
Anti-inflammatory, analgesic, and ulcerogenic properties, and in vitro nitric oxide releasing characteristic of a hybrid molecule which has an indomethacin like structure, oxadia. Anti-inflammatory effects (inhibitory effects on the cox enzyme) than parent aspirin 136 , and showed a better ros scavenging activity than the versatile antioxidant, tempol 102. Celecoxib (13) and rofecoxib (17) analogues, in which the respective so 2 nh 2 and so 2 me hydrogen-bonding pharmacophores were replaced by a dipolar azido bioisosteric substituent, were investigated.
Abstracta series of novel hybrid quinazoline-triazine derivatives was designed and synthesized from cyanuric chloride and anthranilic acid through sequential reactions, which contain different pharmacophores like quinazoline and substituted diaryl triazine (data) linked with ethylene diamine. Proposed strategy towards azt-betulinic acid hybrid molecules as potential anti-hiv agents makes it possible to vary the c-3 and c-28 pharmacophores in triterpene moieties the c-2 propargyl-substituted betulinic acid. Indomethacin indocin, indocin-sr (discontinued brand in us) is a nonsteroidal anti-inflammatory (nsaid) drug prescribed for the treatment of inflammation caused by gouty arthritis, osteoarthritis, soft tissue injuries such as bursitis and tendinitis, rheumatoid arthritis, and ankylolsing spondylitis. Many of these agents are hybrid molecules designed through concept of molecular hybridization and have shown multiple pharmacological activities the present review compiles research reports on development of different c3-coumarin hybrids.