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Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
The synthesis and structure-activity relationships of a class of tetracyclic butyrophenones that exhibit potent binding affinities to serotonin 5-HT(2A) and dopamine D2 receptors are reported, which led to the discovery of ITI-007, which is a potent 5- HT( 2A) antagonist, postsynaptic D2 antagonist, and inhibitor of serotonin transporter.
Development of a New Type of Protease Inhibitors, Efficacious against FIV and HIV Variants
Based on the structural analysis of FIV protease and drug-resistant HIV proteases and molecular modeling, a new type of inhibitors with a small P3 residue has been developed. These inhibitors are
Alteration of Substrate and Inhibitor Specificity of Feline Immunodeficiency Virus Protease
The data suggest that FIV protease prefers a hydrophobic P2/P2′ residue like Val over Val over Asn or Glu, which are utilized by HIV-1 protease, and that S2/S2′ might play a critical role in distinguishing FIV and HIV- 1 protease by specificity.
Analysis of the S 3 and S 3 * subsite specificities of feline immunodeficiency virus ( FIV ) protease : Development of a broad-based protease inhibitor efficacious against FIV , SIV , and HIV in
The findings suggest that inhibitors with small P3 residue may be efficacious against a broad range of HIV variants as well as interspecies PRs and may contribute to the understanding of HIV resistance to protease inhibitors.
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.