| 词条 | BI 224436 |
| 释义 |
| IUPAC_name = (2S)-[4-(2,3-Dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methyl-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid | image = BI 224436.svg | CAS_number = 1155419-89-8 | PubChem = 66561902 | DrugBank = | ChemSpiderID = 32698770 | UNII = 99A996378Y | ATCvet = | ATC_prefix = none | ATC_suffix = | C=27 | H=26 | N=2 | O=4 | molecular_weight = 442.515 g/mol | smiles = CC1=NC2=CC=CC=C2C(=C1[C@@H](C(=O)O)OC(C)(C)C)C3=C4C5=C(C=C3)OCCC5=CC=N4 | StdInChI = 1S/C27H26N2O4/c1-15-21(25(26(30)31)33-27(2,3)4)23(17-7-5-6-8-19(17)29-15)18-9-10-20-22-16(12-14-32-20)11-13-28-24(18)22/h5-11,13,25H,12,14H2,1-4H3,(H,30,31)/t25-/m0/s1 | StdInChIKey = MIXIIJCBELCMCZ-VWLOTQADSA-N | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Investigational | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = 7 hrs (simulated)[1] | excretion = }}BI 224436 was an investigational new drug under development for the treatment of HIV infection. BI 224436 is the first non-catalytic site integrase inhibitor (NCINI). It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct in its mechanism of action compared to raltegravir and elvitegravir, which bind at the catalytic site.[2] In October 2011, Gilead Sciences purchased exclusive rights to develop BI 224436 and several related compounds under investigation in Boehringer Ingelheim’s noncatalytic site integrase inhibitor program.[3][4] Clinical trials were abandoned in advance of Phase 1.[5] References1. ^Pharmacodynamics of BI 224436 for HIV-1 in an in vitro hollow fiber infection model system {{Antiretroviral drug}}{{antiinfective-drug-stub}}2. ^Levin, Jules. BI 224436, a Non-Catalytic Site Integrase Inhibitor, is a potent inhibitor of the replication of treatment-naïve and raltegravir-resistant clinical isolates of HIV-1. Conference Reports for NATAP. ICAAC Chicago Sept 17-20 2011. 3. ^Gilead Negotiates Worldwide License to BI’s Early Clinical Stage HIV Program. Genetic Engineering and Biotechnology News. 6 Oct 2011. 4. ^Highleyman, Liz. ICAAC: New Integrase Inhibitor BI 224436 Active against Raltegravir-Resistant HIV. HIVandHepatitis.com. 7 Oct 2011. 5. ^[https://aidsinfo.nih.gov/clinical-trials/details/NCT01276990 Safety and Pharmacokinetics of Multiple Rising Oral Doses of BI 224436 in Healthy Male Volunteers] 3 : Integrase inhibitors|Experimental drugs|Tert-butyl compounds |
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