Nonsteroidal Antiinflammatory and Antiarthritic Drugs

Gund, Peter; Jensen, N. P.

doi:10.1016/b978-0-12-695150-9.50011-8

Cited by 9 publications

(12 citation statements)

References 71 publications

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“…Since then a large body of experimental evidence has accumulated, but nevertheless the structural requirements of NSAID activity or even reliable quantitative structure-activity relationships (QSAR) are still lacking [4]. A complicating factor is the observation that the locus of competitive binding is not only the catalytic site of cyclooxygenase, but also a supplementary site distinct from, but related to, the catalytic site [5].…”

Section: Introductionmentioning

confidence: 99%

Interaction model for the antiinflammatory action of benzoic and salicylic acids and phenols

Mehler

Gerhards

1989

Int J of Quantum Chemistry

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Ab initio, quantum chemical methods have been used to develop an interaction model for the binding of benzoic and salicylic acids and phenols to cyclooxygenase, leading to their antiinflammatory action. The model is based on a regression analysis of the energy of the highest occupied molecular orbital with the potency of the active substances to inhibit prostaglandin production in mouse macrophages and on an analysis of the frontier orbital charge distributions and electrostatic potentials of active and inactive compounds. The model suggests that binding is controlled by an electrostatic orientational factor and a charge transfer or polarization contribution. The observed relative potencies of the phenols and acids can be rationalized with the help of the proposed interaction model.

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Section: Introductionmentioning

confidence: 99%

Interaction model for the antiinflammatory action of benzoic and salicylic acids and phenols

Mehler

Gerhards

1989

Int J of Quantum Chemistry

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“…In this context, we decided to investigate two profusely employed NSAIDs named Indomethacin (IMTC) and Diflunisal (DFNS) (For structural formulae of the NSAIDs see Table ), in connection with their possible scavenging action towards photogenerated ROS. Both IMTC, an indolic acid derivative, and DFNS, a salicylic acid derivative, are NSAIDs widely used due to their anti‐inflammatory and analgesic properties . Nevertheless several NSAIDs, especially IMTC, have been reported due to their adverse effects in the human body, particularly related to gastro‐intestinal disorders.…”

Section: Introductionmentioning

confidence: 99%

TheNSAIDs Indomethacin and Diflunisal as Scavengers of Photogenerated Reactive Oxygen Species

Purpora

Massad

Ferrari

et al. 2013

Photochem & Photobiology

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Diflunisal (DFNS) and Indomethacin (IMTC) are two profusely employed NSAIDs that provide anti-inflammatory and analgesic effects in humans. The scavenging of reactive oxygen species (ROS) by both NSAIDs was systematically studied in pH 7 aqueous solution. The ROS O2 ((1)Δg), O2(•-) and H2O2, generated by visible light irradiation of Riboflavin (Rf) in the presence of DFNS and IMTC, are deactivated by the NSAIDs. The ROS scavenging action by both NSAIDs constitutes an interesting result and adds one more positive aspect to the beneficial actions attributed to these drugs. Nevertheless it should be taken into account that several NSAIDs, in particular IMTC, have been connected to the pathogenesis of gastric mucosal lesions, which in some cases includes ROS generating-ability. DFNS quenches ROS in a dominant physical fashion. It constitutes an excellent protective-antioxidant provided that is practically not destroyed/oxidized after the ROS scavenging action. IMTC, being also an efficient interceptor of ROS, belong to the so-called group of sacrificial-ROS quenchers: It is easily degraded by the oxidative species in the scavenging action. Although this property is negative in the context of prolonged ROS elimination, exhibits a promissory aspect for the degradation of pharmaceutical contaminants, such as NSAIDs, in waste waters.

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“…Its derivatives are of wide interest because of their diverse biological activity and clinical applications (Kazimierczuk et al, 2002). Benzimidazole moiety fulfills the minimum structural requirements that are common for anti-inflammatory compounds (Nicholson et al, 1982); (Gund and Jensen, 1983). It had been reported that many compounds containing benzimidazole moiety possess significant analgesic as well as anti-inflammatory activity (Mertens et al, 1987).…”

Section: Introductionmentioning

confidence: 99%

Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity

2011

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A series of substituted (benzamidostyryl) benzimidazole (3a-r) were synthesized and evaluated for their possible anti-inflammatory and ulcerogenicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Majority of the compounds were active in carrageenaninduced hind paw edema method test and compounds 3b, 3k had shown high potency after 3 and 4 h time intervals (P \ 0.001) almost equipotent to the standard drug indomethacin and showed less severity index than it.

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Nonsteroidal Antiinflammatory and Antiarthritic Drugs

Cited by 9 publications

References 71 publications

Interaction model for the antiinflammatory action of benzoic and salicylic acids and phenols

Interaction model for the antiinflammatory action of benzoic and salicylic acids and phenols

TheNSAIDs Indomethacin and Diflunisal as Scavengers of Photogenerated Reactive Oxygen Species

Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity

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