502487-67-4Relevant articles and documents
Novel polycyclic 'cage'-1,2-diamines as potential anti-tuberculosis agents
Onajole, Oluseye K.,Coovadia, Yacoob,Kruger, Hendrik G.,Maguire, Glenn E.M.,Pillay, Melendhran,Govender, Thavendran
experimental part, p. 1 - 9 (2012/09/08)
A series of polycyclic 'cage' derivatives of N-geranyl-1,2 diamines were synthesized and screened for their anti-mycobacterial activity against H 37Rv, multidrug resistant (MDR) and extensively drug-resistant (XDR) strains of tuberculosis. By substituting the adamantyl skeleton of SQ109 with trishomocubanyl (9), oxa-pentacycloundecyl (14, 16), pentacycloundecyl, PCU, (10, 15) and azapentacycloundecyl (22, 23), the effect of other polycyclic "cage" skeletons could be investigated. Compound 9 (trishomocubanyl moiety) proved to be the most active (MICs: 0.5-2 μg/mL) while PCU hydroxyl derivatives (15 and 23), oxa-pentacycloundecyl and azapentacycloundecyl derivatives displayed similar activity to SQ109 (MICs: 0.5-4 μg/mL) against all three strains of TB used in this study.
Synthesis and evaluation of SQ109 analogues as potential anti-tuberculosis candidates
Onajole, Oluseye K.,Govender, Patrick,Helden, Paul D. van,Kruger, Hendrik G.,Maguire, Glenn E.M.,Wiid, Ian,Govender, Thavendran
experimental part, p. 2075 - 2079 (2010/06/19)
As part of an ongoing project to develop highly potent anti-tuberculosis therapeutics, six SQ109 derivatives were synthesized and screened in vitro for their anti-tuberculosis activity against the ATCC strain H37Rv and the extensively drug-resistant clinical strain XDR 173. Compound 16 with an extended alkene chain was the most active against both strains of Mycobacterium tuberculosis within a MIC range of 0.5-0.25 μM. Compound 12 and SQ109 were potent within a MIC range of 1-0.5 μM, whilst compound 18 displayed an activity within the MIC range of 0.5-2 μM against both Mycobacterium tuberculosis strains.