Arun Divakar Mathiyazhagan, Shanmugam Sivakumar
Department of Organic Chemistry, Madurai Kamaraj University, Madurai, Tamil Nadu, India.
Chem Biol Drug Des. 2017 Oct;90(4):554-560. doi: 10.1111/cbdd.12978. Epub 2017 May 7.
A novel substituted pyrenoylpyrroles was synthesized by the reaction of pyrenoyl chalcone, TosMIC and methyl iodide under mild condition. All the synthesized compounds were screened for their bioactivity, and the MIC was determined, among which few compounds showed moderate antibacterial activity toward Gram-positive as well as Gram-negative bacteria. Further, cytotoxicity assay ascertained that these compounds were non-toxic to mammalian cells as well. The pyrene chromophore in the synthesized compounds (3a-e) and (5a-e) is responsible for the good photophysical properties which have an absorbance at λ 340 nm and emission at λ 410 nm. Hence, two of the selected novel synthesized compounds with non-cytotoxic nature prospected for bio-imaging of bacterial cells using high-content screening analysis show that the molecule is suitable for microbial imaging in pathological diagnostic studies.
在温和条件下，通过芘甲酰查尔酮、TosMIC和碘甲烷的反应合成了一种新型取代芘甲酰吡咯。对所有合成的化合物进行了生物活性筛选，并测定了最低抑菌浓度（MIC），其中少数化合物对革兰氏阳性菌和革兰氏阴性菌均表现出中等抗菌活性。此外，细胞毒性试验确定这些化合物对哺乳动物细胞也无毒。合成化合物（3a - e）和（5a - e）中的芘发色团具有良好的光物理性质，在λ 340 nm处有吸收，在λ 410 nm处有发射。因此，使用高内涵筛选分析对两种具有非细胞毒性性质的新型合成化合物进行细菌细胞生物成像的前景表明，该分子适用于病理诊断研究中的微生物成像。
