Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium

W J Pitts; J W Jetter; D J Pinto; M J Orwat; D G Batt; S R Sherk; J J Petraitis; I C Jacobson; R A Copeland; R L Dowling; B D Jaffee; T L Gardner; E A Jones; R L Magolda

doi:10.1016/s0960-894x(98)00010-9

Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium

Bioorg Med Chem Lett. 1998 Feb 3;8(3):307-12. doi: 10.1016/s0960-894x(98)00010-9.

Authors

W J Pitts¹, J W Jetter, D J Pinto, M J Orwat, D G Batt, S R Sherk, J J Petraitis, I C Jacobson, R A Copeland, R L Dowling, B D Jaffee, T L Gardner, E A Jones, R L Magolda

Affiliation

¹ DuPont Merck Pharmaceutical Company, Wilmington, Delaware 19880-0500, USA.

PMID: 9871675
DOI: 10.1016/s0960-894x(98)00010-9

Abstract

The structure-activity relationships of some tetracyclic heterocycles related to Brequinar were explored. Activities as inhibitors of dihydroorotate dehydrogenase and the mixed lymphocyte reaction are related to ring system, heteroatom placement, and pendant ring substitution.

MeSH terms

Biphenyl Compounds / chemistry*
Dihydroorotate Dehydrogenase
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Heterocyclic Compounds / chemistry*
Heterocyclic Compounds / pharmacology*
Humans
Immunosuppressive Agents / chemistry*
Immunosuppressive Agents / pharmacology*
Lymphocyte Culture Test, Mixed
Oxidoreductases / antagonists & inhibitors
Oxidoreductases Acting on CH-CH Group Donors*
Structure-Activity Relationship

Substances

Biphenyl Compounds
Dihydroorotate Dehydrogenase
Enzyme Inhibitors
Heterocyclic Compounds
Immunosuppressive Agents
brequinar
Oxidoreductases
Oxidoreductases Acting on CH-CH Group Donors