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2004 3
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Page 1
Understanding the binding mode and function of BMS-488043 against HIV-1 viral entry.
Da LT, Quan JM, Wu YD. Da LT, et al. Proteins. 2011 Jun;79(6):1810-9. doi: 10.1002/prot.23005. Epub 2011 Apr 4. Proteins. 2011. PMID: 21465559
A recently discovered small-molecule inhibitor, BMS-488043 (BMS-488), for the invasion of Human immunodeficiency virus Type 1 (HIV-1), shows a high activity against the entry of diversified HIV-1. ...
A recently discovered small-molecule inhibitor, BMS-488043 (BMS-488), for the invasion of Human immunodeficiency virus Type 1 …
Antiviral activity, pharmacokinetics, and safety of BMS-488043, a novel oral small-molecule HIV-1 attachment inhibitor, in HIV-1-infected subjects.
Hanna GJ, Lalezari J, Hellinger JA, Wohl DA, Nettles R, Persson A, Krystal M, Lin P, Colonno R, Grasela DM. Hanna GJ, et al. Antimicrob Agents Chemother. 2011 Feb;55(2):722-8. doi: 10.1128/AAC.00759-10. Epub 2010 Nov 15. Antimicrob Agents Chemother. 2011. PMID: 21078951 Free PMC article. Clinical Trial.
BMS-488043 is a novel and unique oral small-molecule inhibitor of the attachment of human immunodeficiency virus type 1 (HIV-1) to CD4(+) lymphocytes. ...During dosing, four subjects experienced >10-fold reductions in viral susceptibility to BMS-488043 …
BMS-488043 is a novel and unique oral small-molecule inhibitor of the attachment of human immunodeficiency virus type 1 (HIV-1 …
Emerging anti-HIV drugs.
De Clercq E. De Clercq E. Expert Opin Emerg Drugs. 2005 May;10(2):241-73. doi: 10.1517/14728214.10.2.241. Expert Opin Emerg Drugs. 2005. PMID: 15934866 Review.
., reverse transcriptase [NRTIs: PSI-5004, (-)-dOTC, DPC-817, elvucitabine, alovudine, MIV-210, amdoxovir, DOT; NNRTIs: thiocarboxanilide, UC-781, capravirine, dapivirine, etravirine, rilpivirine], protease [PIs: tipranavir, TMC-114]) or other specific viral proteins (i.e., gp120 …
., reverse transcriptase [NRTIs: PSI-5004, (-)-dOTC, DPC-817, elvucitabine, alovudine, MIV-210, amdoxovir, DOT; NNRTIs: thiocarboxanilide, U …
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043).
Kadow JF, Ueda Y, Meanwell NA, Connolly TP, Wang T, Chen CP, Yeung KS, Zhu J, Bender JA, Yang Z, Parker D, Lin PF, Colonno RJ, Mathew M, Morgan D, Zheng M, Chien C, Grasela D. Kadow JF, et al. J Med Chem. 2012 Mar 8;55(5):2048-56. doi: 10.1021/jm201218m. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22356441 Clinical Trial.
BMS-663749, a phosphonooxymethyl prodrug 4 of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043) (2) was prepared and profiled in a variety of preclinical in vitro and in vivo models …
BMS-663749, a phosphonooxymethyl prodrug 4 of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]p …
In vivo patterns of resistance to the HIV attachment inhibitor BMS-488043.
Zhou N, Nowicka-Sans B, Zhang S, Fan L, Fang J, Fang H, Gong YF, Eggers B, Langley DR, Wang T, Kadow J, Grasela D, Hanna GJ, Alexander L, Colonno R, Krystal M, Lin PF. Zhou N, et al. Antimicrob Agents Chemother. 2011 Feb;55(2):729-37. doi: 10.1128/AAC.01173-10. Epub 2010 Nov 15. Antimicrob Agents Chemother. 2011. PMID: 21078948 Free PMC article. Clinical Trial.
A clinical proof-of-concept study of the AI BMS-488043, administered as monotherapy for 8 days, demonstrated significant viral load reductions. ...Thus, our studies demonstrate that although the majority of the subjects' viruses maintained sensitivity to BMS- …
A clinical proof-of-concept study of the AI BMS-488043, administered as monotherapy for 8 days, demonstrated significant viral …
Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase.
Patel RV, Park SW. Patel RV, et al. Bioorg Med Chem. 2015 Sep 1;23(17):5247-63. doi: 10.1016/j.bmc.2015.06.016. Epub 2015 Jun 14. Bioorg Med Chem. 2015. PMID: 26116177 Review.
Such attempts were resulted in a discovery of highly potent anti-HIV agents suitable for clinical trials, for example, BMS-378806, BMS-585248, BMS-626529, BMS-663068, BMS-488043 and BMS-663749, etc. as anti-HIV attachment agents, triciribine, QX432, BI-1 and BI-2 as …
Such attempts were resulted in a discovery of highly potent anti-HIV agents suitable for clinical trials, for example, BMS-378806, BMS-58524 …
The investigations on HIV-1 gp120 bound with BMS-488043 by using docking and molecular dynamics simulations.
Li L, Chen H, Zhao RN, Han JG. Li L, et al. J Mol Model. 2013 Feb;19(2):905-17. doi: 10.1007/s00894-012-1619-5. Epub 2012 Oct 20. J Mol Model. 2013. PMID: 23086459
BMS-488043, like its predecessor BMS-378806, is a small molecule that can block the interactions between gp120 and CD4, and has shown good clinical efficacy. ...Especially, the importance of the hydrophobic groove formed by residues Ile371 and Gly472 which bind B …
BMS-488043, like its predecessor BMS-378806, is a small molecule that can block the interactions between gp120 and CD4, and ha …
Utilization of in vitro Caco-2 permeability and liver microsomal half-life screens in discovering BMS-488043, a novel HIV-1 attachment inhibitor with improved pharmacokinetic properties.
Yang Z, Zadjura LM, Marino AM, D'Arienzo CJ, Malinowski J, Gesenberg C, Lin PF, Colonno RJ, Wang T, Kadow JF, Meanwell NA, Hansel SB. Yang Z, et al. J Pharm Sci. 2010 Apr;99(4):2135-52. doi: 10.1002/jps.21948. J Pharm Sci. 2010. PMID: 19780144
These in vitro characteristics translated well to the in vivo setting. The oral bioavailability of BMS-488043 in rats, dogs, and monkeys was 90%, 57%, and 60%, respectively. ...More importantly, the improvements in preclinical pharmacokinetics translated well to hum …
These in vitro characteristics translated well to the in vivo setting. The oral bioavailability of BMS-488043 in rats, dogs, a …
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activity in HIV-1-infected subjects.
Wang T, Yin Z, Zhang Z, Bender JA, Yang Z, Johnson G, Yang Z, Zadjura LM, D'Arienzo CJ, DiGiugno Parker D, Gesenberg C, Yamanaka GA, Gong YF, Ho HT, Fang H, Zhou N, McAuliffe BV, Eggers BJ, Fan L, Nowicka-Sans B, Dicker IB, Gao Q, Colonno RJ, Lin PF, Meanwell NA, Kadow JF. Wang T, et al. J Med Chem. 2009 Dec 10;52(23):7778-87. doi: 10.1021/jm900843g. J Med Chem. 2009. PMID: 19769332
Optimization of these azaindole leads resulted in the identification of two compounds that were advanced to clinical studies: (R)-1-(4-benzoyl-2-methylpiperazin-1-yl)-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethane-1,2-dione (BMS-377806, 3) and 1-(4-benzoylpiperazin-1-yl)-2-(4, …
Optimization of these azaindole leads resulted in the identification of two compounds that were advanced to clinical studies: (R)-1-(4-benzo …
Identification of human immunodeficiency virus -1 E protein-targeting lead compounds by pharmacophore based screening.
Almehmadi MM, Shafie AA, Allahyani M, Muhammad T, Baammi S, Aljuaid A, Almalki AA, Alsaiari AA, Ashour AA. Almehmadi MM, et al. Saudi Med J. 2022 Dec;43(12):1324-1332. doi: 10.15537/smj.2022.43.12.20220599. Saudi Med J. 2022. PMID: 36517066 Free PMC article.
OBJECTIVES: To identify potential compounds by seeking the knowledge of molecular interactions between human immunodeficiency virus (HIV) glycoprotein (gp) 120 protein and anti-HIV drug (BMS-488043). METHODS: This study is a computational structure-based drug design …
OBJECTIVES: To identify potential compounds by seeking the knowledge of molecular interactions between human immunodeficiency virus (HIV) gl …
26 results