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Literature DB >> 2115589

Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid.

D A Walsh¹, H W Moran, D A Shamblee, W J Welstead, J C Nolan, L F Sancilio, G Graff.

Abstract

A series of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid (amfenac) and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid were synthesized and evaluated for their cyclooxygenase inhibiting properties, antiinflammatory potency, and gastrointestinal irritation liability. One compound, 2-amino-3-(4-chlorobenzoyl)benzeneacetamide, possessed a therapeutic index 1 order of magnitude greater than that of indomethacin.

Entities: Chemical Disease

Mesh：

Substances：

Year: 1990 PMID： 2115589 DOI： 10.1021/jm00170a039

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

7 in total

1. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers.

Authors: T L Ke; G Graff; J M Spellman; J M Yanni
Journal: Inflammation Date: 2000-08 Impact factor: 4.092

2. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy.

Authors: D A Gamache; G Graff; M T Brady; J M Spellman; J M Yanni
Journal: Inflammation Date: 2000-08 Impact factor: 4.092

Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid.

1. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers.

2. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy.

3. QSAR and conformational analysis of the antiinflammatory agent amfenac and analogues.

4. Topical ophthalmic NSAIDs: a discussion with focus on nepafenac ophthalmic suspension.

5. AHR-10037, a non-steroidal anti-inflammatory compound of low gastric toxicity.

6. 3-(4-Chloro-phen-yl)-2,1-benzisoxazole-5-carbonyl chloride.

7. 5-Iodo-3-phenyl-2,1-benzoxazole.