期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 16, 页码 5765-5770出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.03.013
关键词
structure-activity relationship; thieno[2,3-b]pyridine; antiparasite agent; giardiasis
In this work, we performed the design, synthesis, and the structure-activity relationship studies of 13 new derivatives of thieno[2,3-b]pyridine. These derivatives were prepared in high yields (96-70%) and their structures were elucidated by IR, H-1, C-13 NMR, and MS. The biological results showed some derivatives as antiparasitic agents against Giardia lamblia. Computational analysis of HOMO and LUMO energy, HOMO orbital coefficient distribution, electrostatic potential map, dipole moment, and density HOMO was performed to gain insight into the SAR aspects. This study pointed the p-methoxy substituted derivative as a leading compound for the development of new microbicidal medicines based on thieno[2,3-b]pyridine analogs. (c) 2006 Elsevier Ltd. All rights reserved.
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