Browsing by Author "Lee, Yun-Ta"

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Microwave-Assisted Synthesis of Benzimidazole-Linked Indoline and Indole Hybrids from C-2 Linked (o-Aminobenzyl)benzimidazoles
(2018-02-01)
Lee, Yun-Ta
;
Chiu, Feng-Yu
;
Barve, Indrajeet J.
;
Sun, Chung-Ming
;
應用化學系
An efficient and novel synthesis of benzimidazole-linked indoline hybrids via an unconventional Pictet-Spengler-type condensation of C-2 linked (o-aminobenzyl) benzimidazoles with aldehydes and ketones under microwave irradiation has been explored. The key condensation step consists of acid-catalyzed imine generation followed by intramolecular C-C bond formation through unique reactivity of the benzimidazole moiety. The scope of this method is further extended to synthesize tetracyclic pyrroloindole benzimidazole-carboxylates through 2-carboxaldehydes.
Parallel synthesis and biological evolution of quinic acid derivatives as immuno-suppressing agents against T-cell receptors
(2015-01-01)
Huang, Chih-Yu
;
Chen, Li-Hsun
;
Huang, Hsuan-Yu
;
Kao, Feng-Sheng
;
Lee, Yun-Ta
A simple protocol for the synthesis of quinic acid derivatives was established and their biological evolution against T-cells is studied. Results showed that one of the derivatives, Cyn-1324, has low toxicity on T-cells and a high effect on reducing Signal 2 of T-cell immune responses. In vitro binding measurements of atomic force spectroscopy further indicated that the blocking effect of Cyn-1324 between CD28 and CD80 was about 31 + 4%. In vivo animal tests also confirmed that Cyn-1324 can reduce the allergic responses from ovalbumin-induced mice with little toxicity. Based on these observations, Cyn-1324 can be a mild immuno-suppressive candidate for future drug development.