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Paper | Regular issue | Vol 102, No. 5, 2021, pp.900-919
Published online, 25th March, 2021
DOI: 10.3987/COM-21-14422
Synthesis and Evaluation of Dendroamide A and Three Regioisomeric Analogs Having a Reversed Azole Ring as P-Glycoprotein Inhibitors

Takuji Magata, Yoshimi Hirokawa, Yuki Rokuhara, Ryota Nakayama, Rina Takahashi, Masashi Nogami, Yasuto Tai, Tomoki Imahori, Takanori Hashizume, and Naoyoshi Maezaki*

*Faculty of Pharmacy, Osaka Ohtani University, 3-11-1 Nishikiori-Kita, Tondabayashi, Osaka 584-8540, Japan


We have synthesized dendroamide A and three new analogs having a differently oriented azole moiety to reveal the effect of the orientation of the azole rings on the P-glycoprotein inhibitory activity. The appropriate assembly of modified azole units and dimers from natural-type azole units is examined. Although linear trimers including a modified thiazole unit were hard to cyclize compared with a derivative containing a modified oxazole unit, the yields of cyclization were successfully improved by changing the reaction conditions or the position of ring closure. Evaluation of P-glycoprotein inhibitory activity also reported.