Design and synthesis of HIV-1 protease inhibitors.: Novel tetrahydrofuran P2/P2 '-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex

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Design and synthesis of HIV-1 protease inhibitors. : Novel tetrahydrofuran P2/P2 '-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex

QC 20230602
A series of HIV-1 protease inhibitors having new tetrahydrofuran P2/P2' groups have been synthesised and tested for protease inhibition and antiviral activity. Six novel 4-aminotetrahydrofuran derivatives were prepared starting from commercially available isopropylidene-alpha-D-xylofuranose yielding six symmetrical and six unsymmetrical inhibitors. Promising sub nanomolar HIV-1 protease inhibitory activities were obtained. The X-ray crystal structure of the most potent inhibitor (23, K-i 0.25 nM) cocrystallised with HIV-1 protease is discussed and the binding compared with inhibitors 1a and 1b.

Lahmann, Martina,Docent i kemi,1963-Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, S-106 91 Stockholm, Sweden(Swepub:kth)u190mcjj (författare)
Lindberg, J (författare)
Kangasmetsa, J (författare)
Unge, T (författare)
Oscarson, S (författare)
Hallberg, A (författare)
Samuelsson, B (författare)
Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, S-106 91 Stockholm, Sweden (creator_code:org_t)

Ingår i:Bioorganic & Medicinal Chemistry: Elsevier BV11:6, s. 1107-11150968-08961464-3391

Av författaren/redakt...: Oscarsson, K; Lahmann, Martina ...; Lindberg, J; Kangasmetsa, J; Unge, T; Oscarson, S; visa fler...; Hallberg, A; Samuelsson, B; visa färre...

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