Hamish S Sutherland
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Explore the profile of Hamish S Sutherland including associated specialties, affiliations and a list of published articles.
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19
Citations
265
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Recent Articles
1.
Sutherland H, Choi P, Lu G, Giddens A, Tong A, Franzblau S, et al.
Pharmaceuticals (Basel)
. 2022 Sep;
15(9).
PMID: 36145345
Pyrazolo[1,5-]pyrimidines have been reported as potent inhibitors of mycobacterial ATP synthase for the treatment of (). In this work, we report the design and synthesis of approximately 70 novel 3,5-diphenyl--(pyridin-2-ylmethyl)pyrazolo[1,5-]pyrimidin-7-amines...
2.
Choi P, Lu G, Sutherland H, Giddens A, Franzblau S, Cooper C, et al.
Tetrahedron Lett
. 2022 Feb;
90:None.
PMID: 35140452
During our studies into preparing analogues of pyrazolopyrimidine as ATP synthesis inhibitors of , a regiospecific condensation reaction between ethyl 4,4,4-trifluoroacetoacetate and 3-(4-fluorophenyl)-1-pyrazol-5-amine was observed which was dependent on the...
3.
Sutherland H, Lu G, Tong A, Conole D, Franzblau S, Upton A, et al.
Eur J Med Chem
. 2021 Dec;
229:114059.
PMID: 34963068
Drug resistant tuberculsosis (TB) is global health crisis that demands novel treatment strategies. Bacterial ATP synthase inhibitors such as bedaquiline and next-generation analogues (such as TBAJ-876) have shown promising efficacy...
4.
Lu G, Tong A, Conole D, Sutherland H, Choi P, Franzblau S, et al.
Bioorg Med Chem
. 2020 Oct;
28(22):115784.
PMID: 33007562
A series of 5,8-disubstituted tetrahydroisoquinolines were shown to be effective inhibitors of M. tb in culture and modest inhibitors of M. tb ATP synthase. There was a broad general trend...
5.
Choi P, Conole D, Sutherland H, Blaser A, Tong A, Cooper C, et al.
Molecules
. 2020 Apr;
25(6).
PMID: 32245020
Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). Although it shows high efficacy towards drug-resistant forms of TB, its use has...
6.
Sutherland H, Tong A, Choi P, Blaser A, Franzblau S, Cooper C, et al.
Bioorg Med Chem
. 2019 Dec;
28(1):115213.
PMID: 31810890
Analogues of the anti-tuberculosis drug bedaquiline, bearing a 3,5-dimethoxy-4-pyridyl C-unit, retain high anti-bacterial potency yet exert less inhibition of the hERG potassium channel, in vitro, than the parent compound. Two...
7.
Sutherland H, Tong A, Choi P, Blaser A, Conole D, Franzblau S, et al.
Bioorg Med Chem
. 2019 Feb;
27(7):1292-1307.
PMID: 30803745
Bedaquiline is a new drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but has a cardiac liability (prolongation of the QT interval) due...
8.
Blaser A, Sutherland H, Tong A, Choi P, Conole D, Franzblau S, et al.
Bioorg Med Chem
. 2019 Feb;
27(7):1283-1291.
PMID: 30792104
The ATP-synthase inhibitor bedaquiline is effective against drug-resistant tuberculosis but is extremely lipophilic (clogP 7.25) with a very long plasma half-life. Additionally, inhibition of potassium current through the cardiac hERG...
9.
Sutherland H, Tong A, Choi P, Conole D, Blaser A, Franzblau S, et al.
Bioorg Med Chem
. 2018 Feb;
26(8):1797-1809.
PMID: 29482950
Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological...
10.
Choi P, Sutherland H, Tong A, Blaser A, Franzblau S, Cooper C, et al.
Bioorg Med Chem Lett
. 2017 Nov;
27(23):5190-5196.
PMID: 29107541
Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive...