TẠP CHÍ SỐ 2-TV NĂM 2019

Synthesis and bioactivity screening of some novel N-(adamantan-1-yl)-1-aryl-methanimines

Pham Van Hien; Vu Binh Duong; Cao Dang Nam; Nguyen Van Tu; Phan Thi Phuong Dung; Nguyen Quynh Hoa; Phan Dinh Chau

Tóm tắt

Objectives: Synthesis and bioactivity testing of some novel N-(adamantan-1-yl)-1-aryl-methanimines derivatives. Methods: The novel of N-(adamantan-1-yl)-1-aryl-methanimines were synthesized by the condensation of 1-aminoadamantane with aromatic aldehydes in absolute ethanol under the catalyzation of acetic acid. Synthesized compounds were bioactivity tested as inhibition of acetylcholinesterase, antimicrobial, anticancer in vitro. Results: A new series of N-(adamantan-1-yl)-1- aryl-methanimines was designed, synthesized and evaluated for their inhibition of acetylcholinesterase, antimicrobial, anticancer. Representative two compounds did not show the inhibition of acetylcholinesterase and antimicrobials (S. aureus, B. subtilis, L. fermentum, S. enterica, E. coli, P. aureus). However, synthesize compounds were shown to be promising in at least three tumor cell lines with IC50 from 3.6 - 82.2 µg/mL. Otherwise, five per ten compounds possessed the activity against C. albican. Conclusions: At the present work, it had synthesized ten novel N-(adamantan-1-yl)-1-aryl-methanimine derivatives, between them, some compounds were identified against C. albican and with significant cytotoxic activity in testing tumor cell lines. * Keywords: N-(adamantan-1-yl)-1-aryl-methanimines; Bioactivity.

Abstract

Objectives: Synthesis and bioactivity testing of some novel N-(adamantan-1-yl)-1-aryl-methanimines derivatives. Methods: The novel of N-(adamantan-1-yl)-1-aryl-methanimines were synthesized by the condensation of 1-aminoadamantane with aromatic aldehydes in absolute ethanol under the catalyzation of acetic acid. Synthesized compounds were bioactivity tested as inhibition of acetylcholinesterase, antimicrobial, anticancer in vitro. Results: A new series of N-(adamantan-1-yl)-1- aryl-methanimines was designed, synthesized and evaluated for their inhibition of acetylcholinesterase, antimicrobial, anticancer. Representative two compounds did not show the inhibition of acetylcholinesterase and antimicrobials (S. aureus, B. subtilis, L. fermentum, S. enterica, E. coli, P. aureus). However, synthesize compounds were shown to be promising in at least three tumor cell lines with IC50 from 3.6 - 82.2 µg/mL. Otherwise, five per ten compounds possessed the activity against C. albican. Conclusions: At the present work, it had synthesized ten novel N-(adamantan-1-yl)-1-aryl-methanimine derivatives, between them, some compounds were identified against C. albican and with significant cytotoxic activity in testing tumor cell lines. * Keywords: N-(adamantan-1-yl)-1-aryl-methanimines; Bioactivity.

BÀI VIẾT CÙNG SỐ

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