Synthesis and in vitro activity of oleanane type derivatives against Chlamydia trachomatis

IF 1.7 Q3 CHEMISTRY, ORGANIC Organic Communications Pub Date : 2019-09-01 DOI:10.25135/acg.oc.66.19.07.1352
O. Kazakova, L. Rubanik, I. Smirnova, O. Savinova, A. Petrova, N. Poleschuk, E. Khusnutdinova, E. Boreko, Yu. M. Kapustina
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引用次数: 9

Abstract

Modified synthesis of 3β-nicotinoyloxy-olean-12(13)-en-28-oic acid and 3-deoxy-3a-homo-3a-aza28-hydroxy-olean-12(13)-ene from natural occurring oleanolic acid is suggested. These compounds and two others of ursane and lupane type triterpenoids (3-oximino-urs-12-en-28-oic acid and 3-deoxy-3a-homo-3a-aza28-hydroxy-lup-12(13)-ene) were screened in vitro against Chlamydia trachomatis strain F-3271/Belarus/2015. Oleanane triterpenoids became the leading compounds with chemotherapeutic index > 8 and were chosen for further research.
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齐墩烷型衍生物的合成及体外抗沙眼衣原体活性研究
以天然齐墩果酸为原料,改进合成了3β-烟酰氧基-贫-12(13)-烯-28-酸和3-脱氧-3a-同型-3a-氮杂28-羟基-贫-12-烯。这些化合物以及另外两种ursane和lupane型三萜类化合物(3-氧氨基-urs-12-en-28-酸和3-脱氧-3a-同源-3a-氮杂28-羟基-lup-12(13)-ene)在体外对沙眼衣原体菌株F-3271/白俄罗斯/2015进行了筛选。Oleanane三萜类化合物成为化疗指数>8的先导化合物,并被选择用于进一步研究。
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来源期刊
Organic Communications
Organic Communications CHEMISTRY, ORGANIC-
CiteScore
2.80
自引率
11.80%
发文量
21
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