Tuftsin, Thr-Lys-Pro-Arg

Fridkin, Mati; Gottlieb, Philip A.

doi:10.1007/978-94-009-8030-3_9

Cited by 10 publications

(2 citation statements)

References 88 publications

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“…Gans et al reported that Dup 697 is a potent orally effective antiinflammatory agent with less toxicity due to tissue selective inhibition of PG synthesis.5 NE-19550 and NE-28345 are orally active antiinflammatory analgesics derived from the f Part 1 in a series of New Antiinflammatory Agents is ref 7. Scheme I capsaicin class and do not act like conventional NSAIDs via suppression of arachidonic acid metabolism.6 (1) Silber, R. H.; Busch, R. D.; Oslaps, R. Practical Procedure for Estimation of Corticosteron or Hydrocortisone. Clin.…”

Section: Introductionmentioning

confidence: 99%

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New antiinflammatory agents. 2. 5-Phenyl-3H-imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones: a new class of nonsteroidal antiinflammatory agents with potent activity like glucocorticoids

Suzuki

Kuroda²,

Tamura³

et al. 1992

J. Med. Chem.

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We previously described new antiinflammatory agents, 4-hydroxy-2-oxo-1-phenyl-1H-1,8-naphthyridine-3-carboxamides 1. Further modification of the compounds bearing 1-phenyl-1,8-naphthyridin-2-one as a mother skeleton led to 5-phenylimidazo[4,5-c][1,8]naphthyridin-4(5H)-one derivatives 2 and 3. Regioselective synthesis of these compounds bearing a substituent at the 1- or 3-position was conducted according to the method shown in Schemes I and II. In this series of compounds, antiinflammatory activities were greatly influenced by the position and nature of substituents on imidazole. 3-Alkyl or 3-benzyl substitution result in the potent activity, but 1-substitution did not. Minor modification of the benzyl group reduced or eliminated the activity. Detailed examination of structure-activity relationships led to 3-benzyl-5-phenyl-3H-imidazo[4,5-c][1,8]naphthyridin-4(5H)-one (22), which exhibited potent oral antiinflammatory activities in carrageenan-, zymosan-, and reversed passive Arthus reaction-induced rat paw edemas (ED40 = 5.3, 0.37 mg/kg, ED50 = 0.47 mg/kg, respectively). This broad activity of 22 was like that of glucocorticoids. Compound 22 did not affect activities of CO and 5-LO enzymes and receptor binding of various ligands. As one of the mechanisms of action, induction of release of glucocorticoids was postulated. These results suggest that 22 represents a novel class of antiinflammatory agents.

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Section: Introductionmentioning

confidence: 99%

“…[ 1,8]naphthyridin-4(5fi)-one Derivatives on Carrageenan-, Zymosan-, and Reversed Passive Arthus Reaction-Induced Rat Paw Edemas by the Oral Route…”

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confidence: 99%