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

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Chemical Compound Review:

CHEMBL309896 (4R)-6-chloro-4-cyclopropyl- 4-(2-pyridin-2...

Synonyms: AG-J-91040, SureCN7402060, KST-1A1852, AC1Q3RPD, CTK4D0115, ...

Carroll, S.S. et al., Prueksaritanont, T. et al.

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Disease relevance of L 738372

L-738,372 is a reversible inhibitor of HIV-1 RT and is noncompetitive against dTTP with a Ki of 140 nM with poly(rA).oligo(dT) as primer-template [1].
6-Chloro-(4S)-cyclopropyl-3,4-dihydro-4-((2-pyridyl)-ethynyl)quinazol in- 2(1H)-one (L-738,372) is representative of a novel structural class of nonnucleoside inhibitors of human immunodeficiency virus, strain 1 (HIV-1), reverse transcriptase (RT), the quinazolinones [1].

High impact information on L 738372

Following 0.9 mg/kg iv and 9 mg/kg po doses, systemic blood clearance (CLB) and bioavailability (F) of L-738,372 were species-dependent and inversely related (CLB = 48, 15, and 3 ml/min/kg; F = 6, 62 and 94%, in dogs, rats, and monkeys, respectively) [2].
Incubation of L-738,372 with rat liver slices and liver microsomes from all species studied led to the formation of two hydroxylated metabolites, M1 and M2 [2].

References

Inhibition of HIV-1 reverse transcriptase by a quinazolinone and comparison with inhibition by pyridinones. Differences in the rates of inhibitor binding and in synergistic inhibition with nucleoside analogs. Carroll, S.S., Stahlhut, M., Geib, J., Olsen, D.B. J. Biol. Chem. (1994) [Pubmed]
Species differences in the metabolism of a potent HIV-1 reverse transcriptase inhibitor L-738,372. In vivo and in vitro studies in rats, dogs, monkeys, and human. Prueksaritanont, T., Balani, S.K., Dwyer, L.M., Ellis, J.D., Kauffman, L.R., Varga, S.L., Pitzenberger, S.M., Theoharides, A.D. Drug Metab. Dispos. (1995) [Pubmed]

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