Pyrimidine derivatives with antitubercular activity

被引：48

作者：

Finger, Vladimir ^{[1
,2
]}

Kufa, Martin ^{[1
,2
]}

Soukup, Ondrej ^{[2
]}

Castagnolo, Daniele ^{[3
]}

Roh, Jaroslav ^{[1
]}

Korabecny, Jan ^{[2
]}

机构：

[1] Charles Univ Prague, Fac Pharm Hradec Kralove, Akad Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic

[2] Univ Hosp Hradec Kralove, Biomed Res Ctr, Sokolska 581, Hradec Kralove 50005, Kralove, Czech Republic

[3] UCL, Dept Chem, 20 Gordon St, London WC1H 0AJ, England

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2023年 / 246卷

关键词：

Mycobacterium tuberculosis; Pyrimidine; Tuberculosis; Drug development; Structure-activity relationships; KILL MYCOBACTERIUM-TUBERCULOSIS; THYMIDINE MONOPHOSPHATE KINASE; CYTOCHROME BC(1) COMPLEX; D-RIBOSE 2'-EPIMERASE; ANTIMYCOBACTERIAL ACTIVITY; POTENT INHIBITORS; CRYSTAL-STRUCTURE; COMBINATION THERAPY; DPRE1; INHIBITORS; DRUG DISCOVERY;

D O I：

10.1016/j.ejmech.2022.114946

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.

引用

页数：17

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