154458-56-7Relevant academic research and scientific papers
Synthesis and immunological study of a wall teichoic acid-based vaccine against E. faecium U0317
Zhou, Zhifang,Ding, Wenzhang,Li, Chen,Wu, Zhimeng
, p. 205 - 219 (2017/11/15)
A repeat unit of cell wall teichoic acids (WTA) isolated from E. faecium U0317 was chemically synthesized efficiently by a stepwise strategy. It was derivatized with a 5-aminopentanyl linker to facilitate conjugation with carrier proteins KLH and HSA. Immunological studies of the KLH conjugate 1 demonstrated that it could provoke robust immune responses and high titers of IgG antibodies, which could successfully recognize the synthesized WTA repeat unit 3. This result suggested that synthetic glycoconjugate 1 could be a promising vaccine candidate against E. faecium for further studies.
Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6 S)-2-nitro-6-{[4-(trifluoromethoxy) benzyl]oxy}-6,7-dihydro-5 H -imidazo[2,1- b ][1,3]oxazine (PA-824)
Thompson, Andrew M.,Sutherland, Hamish S.,Palmer, Brian D.,Kmentova, Iveta,Blaser, Adrian,Franzblau, Scott G.,Wan, Baojie,Wang, Yuehong,Ma, Zhenkun,Denny, William A.
experimental part, p. 6563 - 6585 (2011/12/02)
New analogues of antitubercular drug PA-824 were synthesized, featuring alternative side chain ether linkers of varying size and flexibility, seeking drug candidates with enhanced metabolic stability and high efficacy. Both α-methyl substitution and removal of the benzylic methylene were broadly tolerated in vitro, with a biaryl example of the latter class exhibiting an 8-fold better efficacy than the parent drug in a mouse model of acute Mycobacterium tuberculosis infection and negligible fragmentation to an alcohol metabolite in liver microsomes. Extended linkers (notably propenyloxy, propynyloxy, and pentynyloxy) provided greater potencies against replicating M. tb (monoaryl analogues), with propynyl ethers being most effective under anaerobic (nonreplicating) conditions (mono/biaryl analogues). For benzyloxybenzyl and biaryl derivatives, aerobic activity was maximal with the original (OCH2) linker. One propynyloxy-linked compound displayed an 89-fold higher efficacy than the parent drug in the acute model, and it was slightly superior to antitubercular drug OPC-67683 in a chronic infection model.
Compositions containing lysophosphatidic acids which inhibit apoptosis and uses thereof
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Page/Page column 43, (2008/06/13)
The invention provides anti-apoptotic compositions lysophosphatidic acids and methods for making and using the compositions. Such compositions can also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.
Activation of silylphosphines by diethyl azodicarboxylate: Novel silylation of alcohols
Hayashi, Minoru,Matsuura, Yutaka,Watanabe, Yutaka
, p. 1409 - 1411 (2007/10/03)
A novel activation mode of silylphosphines and an application of that to silylation of alcohols were described. Silylphosphines were found to be instantly activated by means of DEAD and PPTS to form reactive silyl cation equivalents. By using the activate
Compositions containing lysophosphotidic acids which inhibit apoptosis and uses thereof
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, (2008/06/13)
The present invention provides therapeutic compositions containing lysophosphotidic acids, methods for making the compositions, and methods of using the compositions in the preservation and treatment of organs.
Microbial asymmetric reduction of α-hydroxyketones in the anti-Prelog selectivity
Tsujigami, Toshikuni,Sugai, Takeshi,Ohta, Hiromichi
, p. 2543 - 2549 (2007/10/03)
Yamadazyma farinosa IFO 10896 was found to reduce α-hydroxyketones bearing a phenyl ring to give optically active diols with anti-Prelog selectivity. The distance between the carbonyl group and the phenyl ring was shown to have an interesting effect on the reactivity and selectivity of the enzyme system.
The synthesis of archaebacterial lipid analogues
Raguse, Burkhard,Culshaw, Peter N.,Prashar, Jognandan K.,Raval, Kiran
, p. 2971 - 2974 (2007/10/03)
An efficient and convenient route to two novel quasimacrocyclic archaebacterial lipid analogues is presented. The target compounds 2 and 3 are prepared in seven and four steps, respectively, from known starting materials, and are useful for the study of s
Nucleoside derivatives and process for preparing thereof
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, (2008/06/13)
PCT No. PCT/KR95/00135 Sec. 371 Date Jun. 11, 1997 Sec. 102(e) Date Jun. 11, 1997 PCT Filed Oct. 21, 1995 PCT Pub. No. WO96/12716 PCT Pub. Date May 2, 1996Nucleoside derivatives represented by formula (I); wherein, R1 represents hydrogen, phosphate or phosphonate group, R2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); wherein, R7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO2, O or C, with a base.
Synthetic studies towards spirostaphylotrichins: Synthesis of building blocks
Steiner,Tamm
, p. 6729 - 6732 (2007/10/02)
A retrosynthetic strategy for the total synthesis of spirostaphylotrichins is presented. The building blocks 7, 8 and 16 were synthesized.
