Stable Tricyclic Antitubercular Ozonides Derived from Artemisinin

被引：40

作者：

Chaudhary, Sandeep ^{[1
,2
,3
]}

Sharma, Vashundhra ^{[1
,2
]}

Jaiswal, Pradeep K. ^{[1
,2
]}

Gaikwad, Anil N. ^{[4
]}

Sinha, Sudhir K. ^{[5
]}

Puri, Sunil K. ^{[6
]}

Sharon, Ashoke ^{[7
]}

Maulik, Prakas R. ^{[7
]}

Chaturvedi, Vinita ^{[5
]}

机构：

[1] Malaviya Natl Inst Technol, Dept Chem, Jaipur 302017, Rajasthan, India

[2] Malaviya Natl Inst Technol, Mat Res Ctr, Jaipur 302017, Rajasthan, India

[3] CSIR, Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226031, Uttar Pradesh, India

[4] CSIR, Cent Drug Res Inst, Div Pharmacol, Lucknow 226031, Uttar Pradesh, India

[5] CSIR, Cent Drug Res Inst, Div Biochem, Lucknow 226031, Uttar Pradesh, India

[6] CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226031, Uttar Pradesh, India

[7] CSIR, Cent Drug Res Inst, Div Mol & Struct Biol, Lucknow 226031, Uttar Pradesh, India

来源：

ORGANIC LETTERS | 2015年 / 17卷 / 20期

关键词：

QINGHAOSU ARTEMISININ; ANTIMALARIAL PEROXIDES; HYDROGEN-PEROXIDE; DERIVATIVES; DRUG; MALARIA; CHEMISTRY; ANTIMYCOBACTERIAL; CANDIDATE; TRIOXANES;

D O I：

10.1021/acs.orglett.5b02296

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

New, highly stable tricyclic antitubercular ozonides 9 and 10 derived from artemisinin are reported in 39 and 9% yields, respectively. The ozonide groups of 9 and 10 were found to be stable under strong basic and acidic conditions. The absolute configuration of ozonides 9 was confirmed by X-ray crystallography. Ozonide 10 shows promising antitubercular activity against M. tuberculosis H37Ra and M. tuberculosis H(37)Rv with MIC values of 0.39 and 3.12 mu g/ml,, respectively.

引用

页码：4948 / 4951

页数：4

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