含环状β-氨基酸的二肽的合成与抗疟活性评价
Synthesis and antimalarial evaluation of cyclic beta-amino acid-containing dipeptides.
作者信息
Sathe Manisha, Thavaselvam Duraipandian, Srivastava Ashish Kumar, Kaushik Mahabir Parshad
机构信息
Discovery Center, Defence R & D Establishment, Jhansi Road, Gwalior 474002, India.
出版信息
Molecules. 2008 Feb 18;13(2):432-43. doi: 10.3390/molecules13020432.
Abstract
This paper describes an efficient synthesis and the antiparasitic evaluation of cyclic beta-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial properties of all these dipeptides have been evaluated in vitro against Plasmodium falciparum and in vivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be very effective in this respect, with IC50 values of 3.87 and 3.64 microg/mL in the in vitro test, while 4.5 has also been found to be active in the in vivo evaluation.
摘要
本文描述了含环β-氨基酸的二肽3.1 - 3.6和4.1 - 4.5的高效合成及其抗寄生虫评估。所有这些二肽的抗疟特性已在体外针对恶性疟原虫进行评估，并在体内针对伯氏疟原虫进行评估。已发现化合物4.4和4.5在这方面非常有效，体外试验中的IC50值分别为3.87和3.64微克/毫升，同时还发现4.5在体内评估中具有活性。
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