Lersivirine - CAS 473921-12-9
Catalog number: 473921-12-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C17H18N4O2
Molecular Weight:
310.35
COA:
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Targets:
HIV
Description:
Lersivirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for the treatment of HIV-1 infection. It prevents HIV from entering the nucleus of healthy CD4 cells, which prevents the cells from producing new virus and decreases the amount of virus in the body.
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Purity:
>98%
Synonyms:
UK-453061
MSDS:
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1.Mild palladium-catalyzed cyanation of (hetero)aryl halides and triflates in aqueous media.
Cohen DT1, Buchwald SL. Org Lett. 2015 Jan 16;17(2):202-5. doi: 10.1021/ol5032359. Epub 2015 Jan 2.
A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.
2.Two-year carcinogenicity study in rats with a nonnucleoside reverse transcriptase inhibitor.
Nambiar PR1, Morton D2, Dochterman LW3, Houle C4, Thomford PJ3, Fate G4, Bailey SA5, Finch GL4. Toxicol Pathol. 2015 Apr;43(3):354-65. doi: 10.1177/0192623314544381. Epub 2014 Aug 13.
Administration of lersivirine, a nonnucleotide reverse transcriptase inhibitor, daily by oral gavage to Sprague-Dawley rats for up to 2 yr was associated with decreased survival, decreased body weights, and an increase in neoplasms and related proliferative lesions in the liver, thyroid, kidney, and urinary bladder. Thyroid follicular adenoma and carcinoma, the associated thyroid follicular hypertrophy/hyperplasia, hepatocellular adenoma/adenocarcinoma, altered cell foci, and hepatocellular hypertrophy were consistent with lersivirine-related induction of hepatic microsomal enzymes. Renal tubular adenoma and renal tubular hyperplasia were attributed to the lersivirine-related exacerbation of chronic progressive nephropathy (CPN), while urinary bladder hyperplasia and transitional cell carcinoma in the renal pelvis and urinary bladder were attributed to urinary calculi. Renal tubular neoplasms associated with increased incidence and severity of CPN, neoplasms of transitional epithelium attributed to crystalluria, and thyroid follicular and hepatocellular neoplasms related to hepatic enzyme induction have low relevance for human risk assessment.
3.The HIV-1 non-nucleoside reverse transcriptase inhibitors (part V): capravirine and its analogues.
Li X1, Zhan P, De Clercq E, Liu X. Curr Med Chem. 2012;19(36):6138-49.
Capravirine (S-1153, AG1549), a 1,2,4,5-tetrasubstituted imidazole derivative, was firstly reported by the Shionogi company to inhibit HIV-1 strains which were resistant to other NNRTIs. However, safety and efficacy studies showed that capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb. Notwithstanding, with aim to obtain novel inhibitors against drug-resistant HIV-1 strains, an in-depth analysis of the particular binding mode of capravirine, together with the wide use of analogue-based chemical evolution strategies, such as bioisosteric replacement, molecular hybridization, prodrug approach, ligand efficiency, etc., gave a huge impetus to the optimization of capravirine. Especially, lersivirine (UK-453,061) was selected for further clinical evaluation due to its very impressive potency against a broad panel of key HIV-1 mutants, safety, pharmacokinetics and other pharmaceutical factors.
4.Efficacy and safety of lersivirine (UK-453,061) versus efavirenz in antiretroviral treatment-naive HIV-1-infected patients: week 48 primary analysis results from an ongoing, multicenter, randomized, double-blind, phase IIb trial.
Vernazza P1, Wang C, Pozniak A, Weil E, Pulik P, Cooper DA, Kaplan R, Lazzarin A, Valdez H, Goodrich J, Mori J, Craig C, Tawadrous M. J Acquir Immune Defic Syndr. 2013 Feb 1;62(2):171-9. doi: 10.1097/QAI.0b013e31827a2ba2..
OBJECTIVE: A 96-week clinical study was planned to estimate the antiviral activity and safety of lersivirine in treatment-naive HIV-1-infected patients.
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CAS 473921-12-9 Lersivirine

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