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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Chemical Compound Review: 

Ici-D2138     6-[[3-fluoro-5-(4- methoxyoxan-4...

Synonyms: CHEMBL20403, AG-D-81587, SureCN1083603, ACMC-20mzth, ZD-2138, ...
 
 
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High impact information on ZD 2138

  • Nonredox type 5-lipoxygenase (5-LO) inhibitors, such as ZM 230487, its methyl analogue ZD 2138, or the Merck compound L-739,010, suppress cellular leukotriene synthesis of ionophore stimulated granulocytes with IC50 values of about 50 nM [1].
  • Furthermore, the cyclization of the ethers has given a highly potent, but achiral series, the methoxytetrahydropyrans (methoxyTHP), exemplified by 41 (ZD-2138) presently under clinical evaluation [2].
  • The reportedly specific inhibitor of 5-lipoxygenase, ZD-2138, substantially inhibited allergen-induced pulmonary bronchoconstriction but did not influence glycoconjugate secretion [3].

References

  1. Nonredox 5-lipoxygenase inhibitors require glutathione peroxidase for efficient inhibition of 5-lipoxygenase activity. Werz, O., Szellas, D., Henseler, M., Steinhilber, D. Mol. Pharmacol. (1998) [Pubmed]
  2. Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series. Lambert-van der Brempt, C., Bruneau, P., Lamorlette, M.A., Foster, S.J. J. Med. Chem. (1994) [Pubmed]
  3. Allergen-induced glycoconjugate secretion in guinea-pig trachea in vivo: modulation by indomethacin, BW B70C and ZD-2138. Yeadon, M., Price, R.C., Payne, A.N. Pulmonary pharmacology. (1995) [Pubmed]
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