Syntheses and biological evaluation of two new naproxen analogs

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 19, 1996, Pages 2281-2282

  Jung, Kyung Woon ^a   Janda, Kim D ^a   Sanfilippo, Pauline J ^b   Wachter, Michael ^b  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

NAPROXEN; NAPROXEN DERIVATIVE; PROSTAGLANDIN SYNTHASE;

ARTICLE; CELL LINE; CONTROLLED STUDY; DRUG SYNTHESIS; ENDOTHELIUM CELL; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; NORMAL HUMAN; REACTION ANALYSIS; THROMBOCYTE;

EID: 0030575628     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00412-X     Document Type: Article

References (11)

1. 1. (a) Shen, T. Y. Annu. Rep. Med. Chem. 1967, 215.
2. (b) Shen, T. Y. Angew. Chem. Int. Ed. Engl. 1972, 11, 460.
3. (c) Sanders, H. J. C&EN 1968, 46 (34), 46.
4. 2. For naproxen and representative analogs, see: (a) Pala, G.; Bruzzese, T.; Marazzi-Uberti, E.; Coppi, G. J. Med. Chem. 1966, 9, 603.
5. (b) Harrison, I. T.; Lewis, B.; Nelson, P.; Rooks, W.; Roszkowski, A.; Tomolonis, A.; Fried, J. H. J. Med. Chem. 1970, 13, 203.
6. For biological evaluation, see: (c) Roszkowski, A. P.; Rooks II, W. H.; Tomolonis, A. J.; Miller, L. M. J. Pharm. Exp. Ther. 1971, 179, 114.
7. (d) Tomlinson, R. V.; Ringold, H. J.; Qureshi, M. C.; Forchielli, E. Biochem. Biophys. Res. Commun. 1972, 46, 552.
8. (e) Brogden, R. N.; Heel, R. C.; Speight, T. M.; Avery, G. S. Drugs 1979, 18, 241.
9. 3; the resulting alcohol was protected as its silyl ether using a combination of TBSCl and imidazole.
10. 2 was measured by radioimmunoassay (RIA).
11. 5. Prostaglandin E2 levels were measured by RIA following the addition of arachidonic acid to cells.