- Total synthesis and structure-activity relationships of new echinocandin-like antifungal cyclolipohexapeptides
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A series of new echinocandin-like cyclolipohexapeptides were designed and total synthesized via solution phase [3 + 3]-segment coupling strategy with an attempt to improve antifungal activity. The designed compounds showed potent antifungal activities with broad spectrum. In particular, 11 compounds (i.e. 28a-e, 28g, 28i-j, 29a, 29c and 29e) showed better in vitro antifungal activities against Candida albicans or Aspergillus fumigatus than caspofungin. Moreover, the synthesized compounds provided new SAR information for the echinocandins. The findings in this work suggested that the "left" tripeptide segment of cyclolipohexapeptide scaffold might be a hydrophilic structural motif, whereas the "right" lipopeptide segment was preferred as a hydrophobic core. The amino acid component of the cyclolipohexapeptide scaffold could significantly affect the SAR of the side chains.
- Yao, Jianzhong,Liu, Hongming,Zhou, Ting,Chen, Hai,Miao, Zhenyuan,Sheng, Chunquan,Zhang, Wannian
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experimental part
p. 196 - 208
(2012/07/28)
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- Synthesis of liquid crystal molecules based on bis(biphenyl)diacetylene and their liquid crystallinity
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We synthesized novel liquid crystalline molecules that contain a bis(biphenyl)diacetylene mesogen and confirmed their structures by 1HNMR, 13CNMR, and FT-IR spectroscopy and mass spectrometry. These compounds formed thermotropic liquid crystals in a wide temperature region that was well characterized by optical microscopic and X-ray measurements.
- Uchimura, Makoto,Kang, Sungmin,Ishige, Rohei,Watanabe, Junji,Konishi, Gen-Ichi
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supporting information; experimental part
p. 513 - 515
(2010/08/20)
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- Cyclic compounds
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The present invention relates to novel Aerothricins represented by the Formula (I), wherein R1, R2, R3, R4, R5, X, Y, Z, and m are as defined in Claim 1; and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition comprising an Aerothricin of the Formula (I) and a pharmaceutically acceptable carrier. Furthermore, the present invention relates to the use of such Aerothricins for the preparation of medicaments, as well as to processes and intermediates for the preparation of the Aerothricins of the Formula (I).
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- Intranasal cyclic peptide formulations
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The present invention relates to a nasally administrable composition of a physiologically active cyclic peptide and pharmaceutically acceptable salts thereof that is prepared by homogeneously dispersing a physiologically active cyclic peptide such as antifungal cyclic peptides (aerothricins, echinocandin analogs, pneumocandin analogs, and aureobacidines), antibacterial cyclic peptides (e.g. vancomycin, daptomycin), cyclosporin A, lanreotide, vapreotide, vasopressin antagonist (U.S. Pat. No. 5,095,003) and eptifibatide in unique carrier, i.e. a physiologically acceptable powdery or crystalline carrier containing a water insoluble polyvalent metal carrier, or organic carrier having a mean particle size of 20 to 500 μm, in the presence or absence of an absorption enhancer and by homogeneously adsorbing onto the carrier, and its use for therapeutic treatment of disease such as systemic fungal infections by intranasal administration. The composition can be nasally administered in powder form.
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- Synthesis and property of liquid crystalline 4-alkoxyl-4″-cyano-p-terphenyls
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The synthesis of some new 4-alkoxyl-4″-cyano-p-terphenyls is described. The preliminary characterization by means of polarized optical microscopy, differential scanning calorimetry and X-ray diffraction shows that all these compounds are thermotropically liquid-crystalline and can form both the nematic and smectic mesophases.
- Zang, Zhi-Qian,Zhang, Dong,Wan, Xin-Hua,Zhou, Qi-Feng
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p. 145 - 158
(2007/10/03)
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