- Rhenium complexes of bidentate, bis-bidentate and tridentate N-heterocyclic carbene ligands
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A series of eight Rhenium(i)-N-heterocyclic carbene (NHC) complexes of the general form [ReCl(CO)3(C^C)] (where C^C is a bis(NHC) bidentate ligand), [ReCl(CO)3(C^C)]2 (where C^C is a bis-bidentate tetra-NHC ligand) and [Re(CO)3(C^N^C)]+[X]- (where C^N^C is a bis(NHC)-amine ligand and the counter ion X is either the ReO4- or PF6-) have been synthesised using a Ag2O transmetallation protocol. The novel precursor imidazolium salts and Re(i) complexes were characterized by elemental analysis, 1H and 13C NMR spectroscopy and the molecular structures for two imidazolium salt and six Re(i) complexes were determined by single crystal X-ray diffraction. These NHC ligand systems are of interest for possible applications in the development of Tc-99m or Re-186/188 radiopharmaceuticals and as such the stability of two complexes of the form [ReCl(CO)3(C^C)] and [Re(CO)3(C^N^C)][ReO4] were evaluated in ligand challenge experiments using the metal binding amino acids l-histidine or l-cysteine. These studies showed that the former was unstable, with the chloride ligand being replaced by either cysteine or histidine, while no evidence for transchelation was observed for the latter suggesting that bis(NHC)-amine ligands of this type may be suitable for biological applications.
- Chan, Chung Ying,Barnard, Peter J.
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- Tightly Bound Double-Caged [60]Fullerene Derivatives with Enhanced Solubility: Structural Features and Application in Solar Cells
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A series of novel highly soluble double-caged [60]fullerene derivatives were prepared by means of lithium-salt-assisted [2+3] cycloaddition. The bispheric molecules feature rigid linking of the fullerene spheres through a four-membered cycle and a pyrrolizidine bridge with an ester function CO2R (R=n-decyl, n-octadecyl, benzyl, and n-butyl; compounds 1 a–d, respectively), as demonstrated by NMR spectroscopy and X-ray diffraction. Cyclic voltammetry studies revealed three closely overlapping pairs of reversible peaks owing to consecutive one-electron reductions of fullerene cages, as well as an irreversible oxidation peak attributed to abstraction of an electron from the nitrogen lone-electron pair. Owing to charge delocalization over both carbon cages, compounds 1 a–d are characterized by upshifted energies of frontier molecular orbitals, a narrowed bandgap, and reduced electron-transfer reorganization energy relative to pristine C60. Neat thin films of the n-decyl compound 1 a demonstrated electron mobility of (1.3±0.4)×10?3 cm2 V?1 s?1, which was comparable to phenyl-C61-butyric acid methyl ester (PCBM) and thus potentially advantageous for organic solar cells (OSC). Application of 1 in OSC allowed a twofold increase in the power conversion efficiencies of as-cast poly(3-hexylthiophene-2,5-diyl) (P3HT)/1 devices relative to the as-cast P3HT/PCBM ones. This is attributed to the good solubility of 1 and their enhanced charge-transport properties — both intramolecular, owing to tightly linked fullerene cages, and intermolecular, owing to the large number of close contacts between the neighboring double-caged molecules. Test P3HT/1 OSCs demonstrated power-conversion efficiencies up to 2.6 % (1 a). Surprisingly low optimal content of double-caged fullerene acceptor 1 in the photoactive layer (≈30 wt %) favored better light harvesting and carrier transport owing to the greater content of P3HT and its higher degree of crystallinity.
- Brotsman, Victor A.,Ioutsi, Vitaliy A.,Rybalchenko, Alexey V.,Markov, Vitaliy Yu.,Belov, Nikita M.,Lukonina, Natalia S.,Troyanov, Sergey I.,Ioffe, Ilya N.,Trukhanov, Vasiliy A.,Galimova, Galina K.,Mannanov, Artur A.,Zubov, Dmitry N.,Kemnitz, Erhard,Sidorov, Lev N.,Magdesieva, Tatiana V.,Paraschuk, Dmitry Yu.,Goryunkov, Alexey A.
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- Synthesis of novel all-cis-functionalized cyclopropane template-assembled collagen models
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An all-cis-functionalized cyclopropane template to connect the three peptide chains in a collagen model is designed. Stereoselective synthesis of cyclopropane-assembled collagen-model 2b with the minimum unit of Gly-Pro-Pro is based on a novel 1-seleno-2-silylethene [2 + 1] cycloaddition strategy. Reaction of the 1-seleno-2-silylethene 4 with triester-substituted olefin 5 in the presence of ZnI2 gives [2 + 1] cycloadduct 6 stereoselectively. Cyclopropane 6 is selectively transformed into triol 10 in four steps. The reaction of 10 and three equivalents ofN-Boc-Pro-Pro-Gly-OH in the presence of WSC-DMAP and subsequent deprotection with TFA gives 2b.
- Yamazaki,Sakamoto,Suzuri,Doi,Nakazawa,Kobayashi
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Read Online
- Discovery of Potent, Reversible, and Competitive Cruzain Inhibitors with Trypanocidal Activity: A Structure-Based Drug Design Approach
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A virtual screening conducted with nearly 4?000?000 compounds from lead-like and fragment-like subsets enabled the identification of a small-molecule inhibitor (1) of the Trypanosoma cruzi cruzain enzyme, a validated drug target for Chagas disease. Subsequent comprehensive structure-based drug design and structure-activity relationship studies led to the discovery of carbamoyl imidazoles as potent, reversible, and competitive cruzain inhibitors. The most potent carbamoyl imidazole inhibitor (45) exhibited high affinity with a Ki value of 20 nM, presenting both in vitro and in vivo activity against T. cruzi. Furthermore, the most promising compounds reduced parasite burden in vivo and showed no toxicity at a dose of 100 mg/kg. These carbamoyl imidazoles are structurally attractive, nonpeptidic, and easy to prepare and synthetically modify. Finally, these results further advance our understanding of the noncovalent mode of inhibition of this pharmaceutically relevant enzyme, building strong foundations for drug discovery efforts.
- De Souza, Mariana L.,De Oliveira Rezende Junior, Celso,Ferreira, Rafaela S.,Espinoza Chávez, Rocio Marisol,Ferreira, Leonardo L. G.,Slafer, Brian W.,Magalh?es, Luma G.,Krogh, Renata,Oliva, Glaucius,Cruz, Fabio Cardoso,Dias, Luiz Carlos,Andricopulo, Adriano D.
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p. 1028 - 1041
(2019/12/27)
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- Double-caged fullerene acceptors: Effect of alkyl chain length on photovoltaic performance
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We report the synthesis and spectroscopic and electrochemical characterization of the benzyl, C4, C6, C8, C9, C10, and C18n-alkyl esters of double-caged fullerene compounds (dFR). Counterintuitively, their solubility depends nonmonotonically on the alkyl chain length with a minimum at n-octyl. The series of dFR compounds were tested in organic solar cells (OSCs) as an acceptor material blended with the poly(3-hexylthiophene-2,5-diyl) (P3HT) donor. With the exception of the n-octadecyl derivative, the performance of the P3HT/dFR solar cells correlates with the solubility of the dFR component, likely due to the improved bulk heterojunction morphology and its favorable effect on JSCvia lower series resistance. A peak PCE of 3.0% was found for the n-nonyl compound, thus exceeding other known fullerene oligomers with fused fullerene cages or cross-linked fullerene dimers. The poor performance of compounds with too long alkyl chains like n-octadecyl reflects larger series resistance that results from a higher degree of phase segregation.
- Brotsman, Victor A.,Rybalchenko, Alexey V.,Zubov, Dmitry N.,Paraschuk, Dmitry Yu.,Goryunkov, Alexey A.
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supporting information
p. 3278 - 3285
(2019/03/19)
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- Synthetic Marine Sponge Collagen by Late-Stage Dihydroxylation
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Based on the observation that an increased substrate size is paralleled by an enhanced diastereoselectivity, a late-stage dihydroxylation protocol toward the 21mer CMP (collagen model peptide) Ac-(Pro-Hyp-Gly)3-Pro-Dyp-Gly-(Pro-Hyp-Gly)3-NH2 is presented. C3 and C4 hydroxylation have a converse effect on the triple-helical stability of collagen. Their combined influence on the melting temperature was studied by NMR spectroscopy.
- Priem, Christoph,Geyer, Armin
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supporting information
p. 162 - 165
(2018/01/17)
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- Preparation method of glycine benzyl ester toluene-4-sulfonate
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The invention discloses a preparation method of glycine benzyl ester toluene-4-sulfonate. The preparation method comprises the steps of carrying out heating reflux after mixing p-toluene sulfonic acid monohydrate or p-toluene sulfonic acid tetrahydrate with methyl benzene, and separating generated water during reflux until no water is generated; then adding glycine and benzyl alcohol in a feed liquid, continuously carrying out heating reflux until no water is generated, separating the generated water, and continuously carrying out the reflux for 1.5 to 2.5 hours; then cooling, stirring and crystallizing, and filtering, washing and drying a crystal substance, thus obtaining a product. According to the preparation method disclosed by the invention, the water contained in p-toluene sulfonic acid is firstly separated, then the generated water can be continuously separated during continuous reaction processes by adding the glycine and the benzyl alcohol, and the reaction is enabled to proceed quickly, so that the reaction time is shortened, and the working efficiency is increased; meanwhile, the yield is increased, and the product quality is also increased.
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Paragraph 0020; 0021
(2016/11/17)
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- C-F Activation in Perfluorinated Arenes with Isonitriles under UV-Light Irradiation
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Due to the great value of fluorinated arenes in agrochemistry, medicinal chemistry and materials science, development of methods for preparation of fluorinated arenes is of high importance. They can be either accessed by arene fluorination or by partial arene defluorination. However, the carbon-fluorine bond belongs to the strongest σ-bonds, which renders C-F activation highly challenging. Here it is shown that aryl and alkyl isonitriles efficiently activate the strong C-F bond in perfluoroarenes by simple UV irradiation under mild conditions. Reactions proceed by formal direct insertion of the isonitrile into the C-F bond without any transition metal. Activation occurs at arene C-F bonds whereas aliphatic C-F bonds remain unreacted. For selected perfluoroarenes C-F activation occurs with high regioselectivity and resulting imidoyl fluorides are transformed into other valuable compounds. Theoretical studies give insights into the reaction mechanism.
- Dewanji, Abhishek,Mück-Lichtenfeld, Christian,Bergander, Klaus,Daniliuc, Constantin G.,Studer, Armido
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supporting information
p. 12295 - 12298
(2015/08/25)
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- A cation-directed two-component cascade approach to enantioenriched pyrroloindolines
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A cascade approach to complex pyrroloindolines bearing all-carbon quaternary stereocentres has been developed. This two-component process uses a chiral ammonium salt to control diastereo- and enantioselectivity in the addition of isocyanides to functionalized alkenes to afford pyrroloindolines with up to three stereocentres. A mechanistic proposal involving intramolecular hydrogen bond activation of the isocyanide is described.
- Wolstenhulme, Jamie R.,Cavell, Alex,Grediak, Matija,Driver, Russell W.,Smith, Martin D.
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supporting information
p. 13585 - 13588
(2015/02/19)
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- Synthesis of NO-NSAID dendritic prodrugs via Passerini reaction:new approach to the design of dendrimer-drug conjugates
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We report the synthesis of a novel class of dendritic prodrugs via Passerini reaction in one pot. Such dendrimers feature a simultaneous attachment of a conventional non-steroidal anti-inflammatory drug (NSAID) (such as ibuprofen and aspirin) and a nitric oxide (NO)-releasing moiety (such as an organic nitrate) onto their surface, and are therefore regarded as new drug delivery systems for NO-releasing NSAIDs (NO-NSAIDs).
- Du, Zuyin,Yanhui, Lu,Dai, Xuedong,Zhang-Negrerie, Daisy,Gao, Qingzhi
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p. 181 - 185
(2013/07/05)
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- Light-driven electron transfer between a photosensitizer and a proton-reducing catalyst Co-adsorbed to NiO
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While intermolecular hole-hopping along the surface of semiconductors is known, there are no previous examples of electron-hopping between molecules on a surface. Herein, we present the first evidence of electron transfer from the photoreduced sensitizer Coumarin-343 (C343) to complex 1, both bound on the surface of NiO. In solution, 1 has been shown to be a mononuclear Fe-based proton-reducing catalyst. The reduction of 1 is reversible and occurs within 50 ns after excitation of C343. Interfacial recombination between the reduced 1(-) and NiO hole occurs on a 100 μs time scale by non-exponential kinetics. The observed process is the first essential step in the photosensitized generation of H2 from a molecular catalyst in the absence of a sacrificial donor reagent.
- Gardner, James M.,Beyler, Maryline,Karnahl, Michael,Tschierlei, Stefanie,Ott, Sascha,Hammarstr?m, Leif
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supporting information
p. 19322 - 19325
(2013/02/22)
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- Asymmetric syntheses and Wnt signal inhibitory activity of melleumin A and four analogues of melleumins A and B
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The first total synthesis of melleumin A and four analogues of melleumins A and B is described. The N-acyl L-Thr-Gly/β-hydroxy-γ-amino acid coupling/macrolactamization strategy allowed the efficient assembly of the three segments being free of epimerization. While the Jouin-Castro method with minor modification allows a rapid entrance to the key syn-β-hy-droxy-y-amino acid segment, required for the synthesis of melleumin A, an extension of our malimide-based methodology using a changed N-protecting group affords a flexible access to several anti-β-hydroxy-γ-amino acids, and hence analogues of melleumins A and B. Among them, unnatural 4-epi-melleumin B (2a) exhibits a modest inhibitory activity on Wnt signaling. The total synthesis of melleumin A allowed confirmation of its full structure.
- Luo, Jie-Min,Dai, Chao-Feng,Lin, Shu-Yong,Huang, Pei-Qiang
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supporting information; experimental part
p. 328 - 335
(2010/04/23)
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- Solution versus fluorous versus solid-phase synthesis of 2,5-disubstituted 1,3-azoles. Preliminary antibacterial activity studies
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(Chemical Equation Presented) A small library of compounds with an oxa(thia)zole scaffold and structural diversity in both positions 2 and 5 has been synthesized. Double acylation of a protected glycine affords intermediate α-amido-β-ketoesters, which in turn can be dehydrated to afford 1,3-oxazoles or reacted with Lawesson's reagent to furnish 1,3-thiazoles. This procedure was designed with its adaptation to fluorous techniques in mind. Thus, when a protected glycine with a fluorous tag in the ester moiety is used as a starting material, the synthesis can be easily completed without column chromatography purification of intermediate compounds with good to excellent yields, thus affording a suitable entry to the preparation of small libraries of these bioactive compounds. The prepared oxa(thia)zoles were assayed for their antibacterial activity, and several of them were active against Staphylococcus aureus.
- Sanz-Cervera, Juan F.,Blasco, Rauel,Piera, Julio,Cynamon, Michael,Ibanez, Ignacio,Murguia, Marcelo,Fustero, Santos
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scheme or table
p. 8988 - 8996
(2010/03/24)
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- Synthesis of chimeric tetrapeptide-linked cholic acid derivatives: Impending synergistic agents
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Tetrapeptides derived from glycine and β-alanine were hooked at the C-3β position of the modified cholic acid to realize novel linear tetrapeptide-linked cholic acid derivatives. All the synthesized compounds were tested against a wide variety of microorganisms (Gram-negative bacteria, Gram-positive bacteria and fungi) and their cytotoxicity was evaluated against human embryonic kidney (HEK293) and human mammary adenocarcinoma (MCF-7) cell lines. While relatively inactive by themselves, these compounds interact synergistically with antibiotics such as fluconazole and erythromycin to inhibit growth of fungi and bacteria, respectively, at 1-24 μg/mL. The synergistic effect shown by our novel compounds is due to their inherent amphiphilicity. The fractional inhibitory concentrations reported are comparable to those reported for Polymyxin B derivatives.
- Bavikar, Sudhir N.,Salunke, Deepak B.,Hazra, Braja G.,Pore, Vandana S.,Dodd, Robert H.,Thierry, Josiane,Shirazi, Fazal,Deshpande, Mukund V.,Kadreppa, Sreenath,Chattopadhyay, Samit
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scheme or table
p. 5512 - 5517
(2009/06/18)
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- Direct anti-selective asymmetric hydrogenation of α-amino-β-keto esters through dynamic kinetic resolution using Ru-axially chiral phosphine catalysts-stereoselective synthesis of anti-β-hydroxy-α-amino acids
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The asymmetric hydrogenation of α-amino-β-keto esters using ruthenium (Ru) anti-selectively proceeds via a dynamic kinetic resolution to afford anti-β-hydroxy-α-amino acids with high enantiomeric purities, which are important chiral building blocks for the synthesis of medicines and natural products. A mechanistic investigation has revealed that the Ru-catalyzed asymmetric hydrogenation takes place via the hydrogenation of the double bond in the enol tautomer of the substrate.
- Makino, Kazuishi,Goto, Takayuki,Hiroki, Yasuhiro,Hamada, Yasumasa
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experimental part
p. 2816 - 2828
(2009/06/28)
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- Configurationally stable propeller-like triarylphosphine and triarylphosphine oxide
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Configurationally stable, propeller-like triarylphosphine and triarylphosphine oxide can be synthesized; a chiral scaffold based on Lissoclinum-cyclopeptides linked via three peptide bonds with a triphenylphosphine and triphenylphosphine oxide moiety, respectively, prevents effectively epimerization at the chiral phosphorus atom. The Royal Society of Chemistry.
- Pinter, Aron,Haberhauer, Gebhard,Hyla-Kryspin, Isabella,Grimme, Stefan
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p. 3711 - 3713
(2008/03/14)
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- PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE BETA-HYDROXY- ALPHA-AMINOCARBOXYLIC ACID DERIVATIVES
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There is provided a process for efficiently producing an anti form of an optically active β-hydroxy-α-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active β-hydroxy-α-aminocarboxylic acid derivative of formula (2) or (3) wherein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, characterized by comprising subjecting an α-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmmetric hydrogenation in the presence of an acid.
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Page/Page column 15-16
(2010/11/08)
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- Synthesis and pharmacological evaluation of side chain modified glutamic acid analogues of the neuroprotective agent glycyl-L-prolyl-L-glutamic acid (GPE)
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The synthesis of eight GPE* analogues, wherein the γ-carboxylic moiety of the glutamic residue has been modified, is described by coupling readily accessible N-benzyloxycarbonyl-glycyl-l-proline with various analogues of glutamic acid. Pharmacological evaluation of the novel compounds was undertaken to further understand the role of the glutamate residue on the observed neuroprotective properties of the endogenous tripeptide GPE.
- Brimble, Margaret A.,Trotter, Nicholas S.,Harris, Paul W.R.,Sieg, Frank
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p. 519 - 532
(2007/10/03)
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- Glycoluril core molecules for combinatorial libraries
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The present invention provides novel glycoluril derivatives for use as core molecules in combinatorial chemistry. Core molecules of the present invention can contain from one to six building blocks. Preferred building blocks are substituted amine radicals. Combinatorial libraries containing such core molecules are also provided.
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- N-acylanilines, herbicide-CHA chimera, and amino acid analogues as novel chemical hybridizing agents for wheat (Triticum aestivum L.)
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In the absence of viable alternative technology of hybrid wheat development, chemical induction of male sterility mediated technology based on chemical hybridizing agents (CHAs) holds a great potential. N-Acylaniline derivatives, namely, ethyl 4′-fluoro oxanilate (1) and ethyl 4′-trifluoromethyl oxanilate (2) containing halogen atoms in the para position of the aryl ring and substituted amide linkage (-CO-NH-) in the acyl side chain induced >98% spikelet sterility on three genotypes of wheat, namely, PBW 343, HD 2046 and HD 2733, at 1500 ppm. The active moieties were incorporated in the form of herbicide-CHA chimera and amino acid analogues using glycine and alanine as templates. The target activity was made more selective by synthesizing chimeric structure of herbicide (2,4-dichlorophenoxyacetic acid and dalapon) and the most active CHA templates, namely, 4-fluoroanilinyl and β-ethoxycarbonyl moieties. Among herbicide-CHA chimera ethyl 2′,4′-dichlorophenyl oxalate (14) induced 79.11% male sterility, whereas benzyl methyl 2-oxo-3-azaadipate (20) was the best, inducing 73.87% male sterility in HD 2733, among amino acid analogues. The CHAs were found to modify the reproductive biology to ensure cross-pollination in the cleistogamous wheat flowers, increasing the probability for the development of hybrids.
- Chakraborty, Kajal,Devakumar
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p. 7899 - 7907
(2007/10/03)
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- SUPRAMOLECULAR COMPOUNDS AND THEIR USE AS ANTITUMOUR AND ANTIVIRAL AGENTS
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The application discloses the use of supramolecular compounds as antitumour, antimicrobial (such as antibacterial and antiprotozoal) and antiviral agents. Such compounds comprise ligands as defined in the application coordinated to at least two metal ions. Pharmaceutical formulations and detergent formulations are also disclosed.
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Page/Page column 76
(2010/02/11)
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- Synthesis of a peptidomimetic HCMV protease inhibitor library
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The human cytomegalovirus (HCMV) protease catalyzes the maturational process of the herpes virus assembly protein and plays a key role during the manufacture of viral capsid, and so is an attractive target for potential anti-herpes-virus agents with novel structures and new mechanisms. In this work, a peptidomimetic skeleton was designed and a chemical library containing 32 compounds with different substitutions on the skeleton was prepared by the oxidation of a precursor library, which was constructed from four types of building blocks: 4 carboxylic acids, 2 amines, 2 aldehydes and 2 isocyanides, based on multicomponent condensation following liquid phase strategies. The syntheses of the key building block isocyanides are presented.
- Xu, Ping,Lin, Wenwei,Zou, Xiaomin
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p. 1017 - 1026
(2007/10/03)
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- A convenient preparation of benzyl 4-(R1)-3-(R2)pyrrole-2-carboxylates
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The class of title pyrroles, important intermediates in porphyrin synthesis, have been prepared via the Barton and Zard method. The benzyl isocyanoacetate used in the synthesis was in turn prepared in an efficient and inexpensive 3-step procedure from glycine.
- Burns,Jabara,Burden
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p. 379 - 387
(2007/10/02)
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- Regioselective synthesis of 5-unsubstituted benzyl pyrrole-2-carboxylates from benzyl isocyanoacetate
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A general synthesis of 5-unsubstituted benzyl pyrrole-2-carboxylates was developed based on the reaction of β-nitroacetates with benzyl isocyanoacetate. The advantage of this route over other pyrrole syntheses was the regiochemical control of the substitution pattern on the pyrrole ring.
- Ono,Katayama,Nisyiyama,Ogawa
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p. 707 - 710
(2007/10/02)
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- Synthesis of pyrroles from benzyl isocyanoacetate
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Benzyl esters of 5-unsubstituted pyrrole-2-carboxylic acids were prepared in excellent yields by the base-catalyzed condensation of benzyl isocyanoacetate with α-acetoxynitro compounds, or nitro-alkenes, in refluxing tetrahydrofuran. These pyrrolic products are important intermediates in the synthesis of porphyrins and related compounds.
- Lash,Bellettini,Bastian,Couch
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p. 170 - 172
(2007/10/02)
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- Synthesis and spectroscopic properties of azaglutamine amino acid and peptide derivatives
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tert-Butyl carbazate and Boc-amino acid hydrazides undergo a Michael addition with acrylamide to give substituted carbazates having the side-chain of glutamine on nitrogen. These carbazates may react with chloroformates to give protected azaglutamine esters, and N-activated amino acid esters to give azaglutamine peptides.
- Gray,Quibell,Jiang,Baggett
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p. 141 - 146
(2007/10/02)
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- AMINOACID DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS
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This invention relates to aminoacid derivatives, and compositions containing the same and having enkephalinase-inhibiting, antalgic, antidiarrhea and hypotensive activities, of the formula STR1 whose variables are as set forth herein, for example STR2
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- Antigen derivatives and processes for their preparation
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The invention relates to novel antigen derivatives comprising an antigen and at least one muramylpeptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine. The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.
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