- Total synthesis and structure-activity relationships of caspofungin-like macrocyclic antifungal lipopeptides
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The echinocandins represent a well-known class of macrocyclic antifungal lipopeptides that can be used for treatment of invasive fungal infections. Due to their complex chemical structures and synthetic difficulties, the structure-activity relationships (SARs) of them are still limited. A total synthetic approach was developed to synthesize structurally diverse caspofungin-like antifungal cyclic lipopeptides, allowing for systemically investigating their SARs. Most of the designed cyclic lipopeptides showed potent antifungal activities with broad spectrum. In particular, several compounds (e.g., 30a, 30e-h, 31a-d, 32c, and 33a,b) were more active in vitro against Candida albicans or Aspergillus fumigatus than caspofungin. The findings in this work indicated that the 'left' tripeptide segment of cyclic lipopeptide scaffold might be suitable for a hydrophilic structural motif, whereas the 'right' lipotripeptide segment was preferred as a hydrophobic core. The alkoxy-naphthoyl was found to be optimal side chain and alkyl length could affect the SARs of alkoxy-aroyl side chains.
- Yao, Jianzhong,Liu, Hongming,Zhou, Ting,Chen, Hai,Miao, Zhenyuan,Dong, Guoqiang,Wang, Shengzheng,Sheng, Chunquan,Zhang, Wannian
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p. 3074 - 3085
(2012/06/01)
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- Donor-acceptor-substituted oligo(1,4-phenylene)s
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Oligo(para-phenylene)s (DAOPPs) 2a-2d (n = 1-4) with terminal donor-acceptor substitution (D = C6H13O, A = NO 2) were prepared by applying Suzuki cross-couplings for chain extension and end capping. The push-pull effect in
- Kim, Soungkyoo,Oehlhof, Annette,Beile, Bernhard,Meier, Herbert
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experimental part
p. 1023 - 1033
(2009/10/16)
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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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