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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, ...
 
 
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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

 
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