Sunduru Naresh, Salin Olli, Gylfe Åsa, Elofsson Mikael
Department of Chemistry, Umeå University, SE90187 Umeå, Sweden; Umeå Centre for Microbial Research (UCMR), SE90187 Umeå, Sweden.
Department of Chemistry, Umeå University, SE90187 Umeå, Sweden; Department of Clinical Microbiology, Umeå University, SE90187 Umeå, Sweden; Umeå Centre for Microbial Research (UCMR), SE90187 Umeå, Sweden.
Eur J Med Chem. 2015 Aug 28;101:595-603. doi: 10.1016/j.ejmech.2015.07.019. Epub 2015 Jul 13.
Discovery of new polypharmacological antibacterial agents with multiple modes of actions can be an alternative to combination therapy and also a possibility to slow development of antibiotic resistance. In support to this hypothesis, we synthesized 16 compounds by combining the pharmacophores of Chlamydia trachomatis inhibitors and inhibitors of type III secretion (T3S) in gram-negative bacteria. In this study we have developed salicylidene acylhydrazide sulfonamides (11c &11d) as new antichlamydial agents that also inhibit T3S in Yersinia pseudotuberculosis.
发现具有多种作用模式的新型多靶点抗菌剂可以替代联合疗法，也有可能减缓抗生素耐药性的发展。为支持这一假设，我们通过结合沙眼衣原体抑制剂和革兰氏阴性菌III型分泌（T3S）抑制剂的药效基团合成了16种化合物。在本研究中，我们开发了水杨醛酰肼磺酰胺（11c和11d）作为新型抗衣原体药物，其也能抑制假结核耶尔森菌中的T3S。
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