نتایج جستجو برای: conformationally restricted
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The non-natural amino acid mesitylalanine (2,4,6-trimethyl-L-phenylalanine; Msa) has an electron-richer and a more conformationally restricted side-chain than that of its natural phenylalanine counterpart. Taking these properties into account, we have synthesized ten somatostatin analogs containing Msa residues in different key positions to modify the intrinsic conformational flexibility of the...
Polyamines cause inward rectification of Kir K(+) channels by blocking deep within the channel pore. We investigated structural constraints of polyamine block of strongly rectifying mutant K(ATP) channels (Kir6.2[L164C,N160D,C166S] + SUR1). We studied three groups of polyamine analogs: 1) conformationally restricted linear tetra-amines with a cycloalkyl or alkene group between the second and th...
The 3-azabicycloACHTUNGTRENNUNG[3.1.0]hexane is a common motif in natural products. Furthermore this rigid framework represents a privileged class of pharmacologically active compounds, often showing enhanced binding affinities with their targets (Figure 1). These bicycles also represent conformationally restricted analogues of piperidines (e.g. trovafloxacin). When substituted with a carboxyli...
This study used thermoelastic measurements to investigate the role of proline in the elastic mechanism of hydrated, spider major ampullate (MA) and flagelliform (FL) silks. Experiments on hydrated MA silk from Araneus diadematus (proline content 16%) reveal that conformational entropy elasticity accounts for about 90% of the elastic force at small extensions, but entropy elasticity drops to abo...
Four novel conformationally restricted (?)-muricatacin analogues, bearing a methoxy group at the C-5 position and with an alkoxymethyl ?s C-7 side chain, have been synthesised their in vitro antiproliferative activity was evaluated against panel of seven human tumour cell lines, as well single normal line. All analogues (9?12) showed diverse effects all tested malignant but were devoid any sign...
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