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Volumn 6, Issue 2, 2011, Pages 253-257

Strategies towards Improving the Pharmacokinetic Profile of ε-Substituted Lysinol-Derived HIV Protease Inhibitors

Author keywords

substituted lysines; HIV; Inhibitors; Pharmacokinetics; Proteases

Indexed keywords

ANILINE DERIVATIVE; BENZYL ALCOHOL DERIVATIVE; HUMAN IMMUNODEFICIENCY VIRUS PROTEINASE INHIBITOR; LYSINE DERIVATIVE; LYSINOL DERIVATIVE; UNCLASSIFIED DRUG;

EID: 79251588434     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201000395     Document Type: Article
Times cited : (7)

References (16)
  • 7
    • 0028222149 scopus 로고
    • 95) is defined as the concentration of agent that inhibits the spread of HIV-1 infection in susceptible cell culture by 95%. MT4 human T-lymphoid cells were maintained in RPMI-1640 medium containing 10% heat-inactivated fetal bovine serum. Cells were infected all together at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24h. At this time, cells were washed and distributed into 96-well microtiter dishes. Serial twofold dilutions of inhibitor were added to the wells, and the cultures were maintained for three additional days. Virus spread was assessed by HIV-1 P24 core antigen ELISA. Control cultures in the absence of inhibitor were fully infected after four days.
    • 95) is defined as the concentration of agent that inhibits the spread of HIV-1 infection in susceptible cell culture by 95%. MT4 human T-lymphoid cells were maintained in RPMI-1640 medium containing 10% heat-inactivated fetal bovine serum. Cells were infected all together at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24h. At this time, cells were washed and distributed into 96-well microtiter dishes. Serial twofold dilutions of inhibitor were added to the wells, and the cultures were maintained for three additional days. Virus spread was assessed by HIV-1 P24 core antigen ELISA. Control cultures in the absence of inhibitor were fully infected after four days.
    • (1994) Proc. Natl. Acad. Sci. USA , vol.91 , pp. 4096-4100
    • Vacca, J.P.1    Dorsey, B.D.2    Schleif, W.A.3    Levin, R.B.4    McDaniel, S.L.5    Darke, P.L.6    Zugay, J.7    Quintero, J.C.8    Blahy, O.M.9    Roth, E.10    Sardana, V.V.11    Schlabac, A.J.12    Graham, P.I.13    Condra, J.H.14    Gotlib, L.15    Holloway, M.K.16    Lin, J.17    Chen, I.-W.18    Vastag, K.19    Ostovic, D.20    more..
  • 8
    • 79251545612 scopus 로고    scopus 로고
    • For the discovery of benzyl alcohols see the following patent, National Institutes of Health; Rockville, USA; University of Illinois, Urbana, USA), WO/1999/067254.
    • For the discovery of benzyl alcohols see the following patent: J. W. Erickson, S. V. Gulnik, A. K. Ghosh, K. A. Hussain, (National Institutes of Health; Rockville, USA; University of Illinois, Urbana, USA), WO/1999/067254, 1999.
    • (1999)
    • Erickson, J.W.1    Gulnik, S.V.2    Ghosh, A.K.3    Hussain, K.A.4
  • 10
    • 79251572182 scopus 로고    scopus 로고
    • A fluorescence resonance energy transfer (FRET)-based assay using HIV protease substrate Ser-Gln-Asn-(β-naphthylalanine)-Pro-Ile-Val.
    • A fluorescence resonance energy transfer (FRET)-based assay using HIV protease substrate Ser-Gln-Asn-(β-naphthylalanine)-Pro-Ile-Val.
  • 11
    • 1442360753 scopus 로고    scopus 로고
    • Handbook of Metathesis
    • Ed.: R.H. Grubbs), Wiley-VCH, Weinheim.
    • Handbook of Metathesis, (Ed.: R.H. Grubbs), Wiley-VCH, Weinheim, 2003.
    • (2003)
  • 12
    • 79251540378 scopus 로고    scopus 로고
    • The diastereomers were separable by silica gel chromatography at stepj in Scheme2 or by preparative HPLC at stepl in Scheme2.
    • The diastereomers were separable by silica gel chromatography at stepj in Scheme2 or by preparative HPLC at stepl in Scheme2.
  • 16
    • 79251552652 scopus 로고    scopus 로고
    • For comparison, the in vitro potency of darunavir (DRV) in our 10% and 50% serum-shifted SPREAD assays are 9 and 23nm, respectively.
    • For comparison, the in vitro potency of darunavir (DRV) in our 10% and 50% serum-shifted SPREAD assays are 9 and 23nm, respectively.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.