Self-Assembly of Bolaamphiphiles Forming Alternating Layer Arrangements with Lead and Copper Divalent Ions
摘要:
Five bifunctional alpha -amino acid-epsilon -carboxy bolaamphiphiles [(2-RS, or RS)-(HOOC)-(CH2)(m)-CONH-(CH2)(n)-CH(COOH)(NH2) m=20,22, n=3,4 labeled (l), (d,l)-C(22)Orn (l), (d), (d,l)-C(22)Lys, (d,l)-C(24)Lys respectively] were synthesized. These molecules were deposited on different aqueous subphases, and studied by means of grazing incidence X-ray diffraction (GIXD). On deionized water, the bolaamphiphiles (dl)-C(22)Lys yield a mixture of crystallites: both a monolayer, in which the chains are tilted from the normal, and a multilayer in which the molecules lie parallel to the water. On the other hand, when deposited on mono- or bi-metal ionic subphases, they self-assemble into crystalline multilayer films in which the molecules lie parallel to the aqueous solution surface, linked head-to-head and tail-to-tail in the form of extended chains. The latter are juxtaposed such that the metal ions form sheets separated by the organic molecules, aligned perpendicular to the plane of the aqueous solution. Deposition of either the enantiomerically pure or racemic bifunctional bolaamphiphiles on an aqueous solution of mixed Cu(Acetate)(2) and Pb(Acetate)(2), yields self-assembled crystalline films composed of the two different metal cations, arranged in alternating sheets, separated by the organic spacer. Both GIXD and X-ray-photoelectric-spectroscopy (XPS) studies (after deposition on solid support) demonstrate that the structures of these films differ form the ones formed on either pure Pb(Ac)(2) or on Cu(AC)(2) solutions, thus excluding the simultaneous formation of the two monometallic crystalline phases.
Pyrrolopyrimidinyalglutaminate derivatives and their use
申请人:Takeda Chemical Industries, Ltd.
公开号:US05403843A1
公开(公告)日:1995-04-04
A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.
INHIBITION OF BACTERIAL BIOFILMS WITH IMIDAZOLE DERIVATIVES
申请人:Melander Christian
公开号:US20080181923A1
公开(公告)日:2008-07-31
Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
INHIBITION OF BIOFILMS IN PLANTS WITH IMIDAZOLE DERIVATIVES
申请人:Melander Christian
公开号:US20090143230A1
公开(公告)日:2009-06-04
Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.
Novel compositions for the delivery of negatively charged molecules
申请人:Ribozyme Pharmaceuticals, Inc.
公开号:US20030073640A1
公开(公告)日:2003-04-17
This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAs, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.
5,11-Dihydro-6H-pyrido[2,3-6][1,4]benzodiazepin-6-one (1), a basic intermediate in the preparation of 11-α-aminoacetyl derivatives with important biological activities, has been obtained by a three-step synthesis starting from easily available isatoic anhydride and anhydro ornithine. Some model cyclisation reactions leading to 5-member ring derivatives 10 and 12 instead of 7-member ring analogues of