Brian D Palmer
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Explore the profile of Brian D Palmer including associated specialties, affiliations and a list of published articles.
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49
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811
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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.
Tijono S, Palmer B, Tomek P, Flanagan J, Henare K, Gamage S, et al.
Pharmaceuticals (Basel)
. 2022 Sep;
15(9).
PMID: 36145311
Indoleamine 2, 3-dioxygenase 1 (IDO1) is commonly expressed by cancers as a mechanism for evading the immune system. Preclinical and clinical studies have indicated the potential of combining IDO1 inhibitors...
3.
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...
4.
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...
5.
Capochiani de Iudicibus R, Tomek P, Palmer B, Tijono S, Flanagan J, Ching L
Bioorg Med Chem
. 2021 Apr;
39:116160.
PMID: 33901770
The expression of tryptophan catabolising enzyme indoleamine 2,3-dioxygenase 1 (IDO1) or tryptophan 2,3-dioxygenase 2 (TDO2) in cancers is associated with suppressed immunity and poor patient prognosis. Results from human clinical...
6.
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...
7.
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...
8.
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...
9.
Kanamala M, Palmer B, Jamieson S, Wilson W, Wu Z
Nanomedicine (Lond)
. 2019 Jul;
14(15):1971-1989.
PMID: 31355712
pH-sensitive liposomes (pSL) have emerged as promising nanocarriers due to their endo/lysosome-escape abilities, however, their pH sensitivity is compromised by poly(ethylene glycol) (PEG) coating. This study investigates whether an intracellular...
10.
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...