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An orally bioavailable HIV-1 protease inhibitor containing an imidazole-derived peptide bond replacement: crystallographic and pharmacokinetic analysis

Autor: S S, Abdel-Meguid, B W, Metcalf, T J, Carr, P, Demarsh, R L, DesJarlais, S, Fisher, D W, Green, L, Ivanoff, D M, Lambert, K H, Murthy

Publikováno v: Biochemistry. 33(39)

(2R,4S,5S,1'S)-2-Phenylmethyl-4-hydroxy-5-(tert-butoxycarbonyl) amino-6-phenylhexanoyl-N-(1'-imidazo-2-yl)-2'-methylpropanamide (compound 2) is a tripeptide analogue inhibitor of HIV-1 protease in which a C-terminal imidazole substituent constitutes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57195bad210ce7eddd3833927d7b2c43
https://pubmed.ncbi.nlm.nih.gov/7918383

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Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere

Autor: S K, Thompson, K H, Murthy, B, Zhao, E, Winborne, D W, Green, S M, Fisher, R L, DesJarlais, T A, Tomaszek, T D, Meek, J G, Gleason

Publikováno v: Journal of medicinal chemistry. 37(19)

The rational design and synthesis of a highly potent inhibitor of HIV-1 protease have been accomplished. The inhibitor, SB 206343, is based on a model derived from the structure of the MVT-101/HIV-1 protease complex and contains a 4(5)-acylimidazole

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::810ff4ecab5086a77f59bc6f9906ada9
https://pubmed.ncbi.nlm.nih.gov/7932533

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Inhibition of human immunodeficiency virus-1 protease by a C2-symmetric phosphinate. Synthesis and crystallographic analysis

Autor: S S, Abdel-Meguid, B, Zhao, K H, Murthy, E, Winborne, J K, Choi, R L, DesJarlais, M D, Minnich, J S, Culp, C, Debouck, T A, Tomaszek

Publikováno v: Biochemistry. 32(31)

The human immunodeficiency virus type 1 (HIV-1) protease is a potential target of acquired immune deficiency syndrome (AIDS) therapy. A highly potent, perfectly symmetrical phosphinate inhibitor of this enzyme, SB204144, has been synthesized. It is a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::977ff3a265eaf6a31672893596b3b42f
https://pubmed.ncbi.nlm.nih.gov/8347601

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The crystal structures at 2.2-A resolution of hydroxyethylene-based inhibitors bound to human immunodeficiency virus type 1 protease show that the inhibitors are present in two distinct orientations

Autor: K H, Murthy, E L, Winborne, M D, Minnich, J S, Culp, C, Debouck

Publikováno v: The Journal of biological chemistry. 267(32)

As part of a structure-based drug design program directed against enzyme targets in the human immunodeficiency virus (HIV), we have determined the three-dimensional structures of the HIV type 1 protease complexed with two hydroxyethylene-based inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ac444d836f2cc3499558c58f0a69a38f
https://pubmed.ncbi.nlm.nih.gov/1429626

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