Search Results - "Sutherland, Hamish S"

Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis by Sutherland, Hamish S., Lu, Guo-Liang, Tong, Amy S.T., Conole, Daniel, Franzblau, Scott G., Upton, Anna M., Lotlikar, Manisha U., Cooper, Christopher B., Palmer, Brian D., Choi, Peter J., Denny, William A.

“…Drug resistant tuberculsosis (TB) is global health crisis that demands novel treatment strategies. Bacterial ATP synthase inhibitors such as bedaquiline and…”
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Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline by Choi, Peter J, Conole, Daniel, Sutherland, Hamish S, Blaser, Adrian, Tong, Amy S T, Cooper, Christopher B, Upton, Anna M, Palmer, Brian D, Denny, William A

“…Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). Although it shows high efficacy towards…”
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Synthesis and Structure–Activity Relationships for the Anti-Mycobacterial Activity of 3-Phenyl-N-(Pyridin-2-ylmethyl)Pyrazolo[1,5-a]Pyrimidin-7-Amines by Sutherland, Hamish S., Choi, Peter J., Lu, Guo-Liang, Giddens, Anna C., Tong, Amy S. T., Franzblau, Scott G., Cooper, Christopher B., Palmer, Brian D., Denny, William A.

“…Pyrazolo[1,5-a]pyrimidines have been reported as potent inhibitors of mycobacterial ATP synthase for the treatment of Mycobacterium tuberculosis (M.tb). In…”
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3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel by Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Blaser, Adrian, Conole, Daniel, Franzblau, Scott G., Lotlikar, Manisha U., Cooper, Christopher B., Upton, Anna M., Denny, William A., Palmer, Brian D.

“…[Display omitted] Bedaquiline is a new drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but…”
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Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles by Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha U., Denny, William A., Palmer, Brian D.

“…[Display omitted] Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing…”
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Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline by Blaser, Adrian, Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha, Denny, William A., Palmer, Brian D.

“…[Display omitted] The ATP-synthase inhibitor bedaquiline is effective against drug-resistant tuberculosis but is extremely lipophilic (clogP 7.25) with a very…”
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Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology by Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha, Denny, William A., Palmer, Brian D.

“…[Display omitted] •Bedaquiline analogues with 3,5-disubstituted-4-pyridyl C-units.•High potency and attenuated hERG inhibition cf bedaquiline.•4–6.5 log units…”
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Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors of Mycobacterium tuberculosis. Structural correction of reported N-(6-(2-(dimethylamino)ethoxy)-5-fluoropyridin-3-yl)-2-(4-fluorophenyl)-5-(trifluoromethyl)pyrazolo[1,5-α]pyrimidin-7-amine by Choi, Peter J., Lu, Guo-Liang, Sutherland, Hamish S., Giddens, Anna C., Franzblau, Scott G., Cooper, Christopher B., Denny, William A., Palmer, Brian D.

“…[Display omitted] During our studies into preparing analogues of pyrazolopyrimidine as ATP synthesis inhibitors of Mycobacterium tuberculosis, a regiospecific…”
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Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units by Choi, Peter J., Sutherland, Hamish S., Tong, Amy S.T., Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Lotlikar, Manisha U., Upton, Anna M., Guillemont, Jerome, Motte, Magali, Queguiner, Laurence, Andries, Koen, Van den Broeck, Walter, Denny, William A., Palmer, Brian D.

“…[Display omitted] Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes,…”
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Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis by Lu, Guo-Liang, Tong, Amy S.T., Conole, Daniel, Sutherland, Hamish S., Choi, Peter J., Franzblau, Scott G., Upton, Anna M., Lotlikar, Manisha U., Cooper, Christopher B., Denny, William A., Palmer, Brian D.

“…[Display omitted] A series of 5,8-disubstituted tetrahydroisoquinolines were shown to be effective inhibitors of M. tb in culture and modest inhibitors of M…”
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Synthesis and Structure−Activity Studies of Biphenyl Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824) by Palmer, Brian D, Thompson, Andrew M, Sutherland, Hamish S, Blaser, Adrian, Kmentova, Iveta, Franzblau, Scott G, Wan, Baojie, Wang, Yuehong, Ma, Zhenkun, Denny, William A

“…A series of biphenyl analogues of the new tuberculosis drug PA-824 was prepared, primarily by coupling the known…”
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6‑Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis by Tong, Amy S. T, Choi, Peter J, Blaser, Adrian, Sutherland, Hamish S, Tsang, Sophia K. Y, Guillemont, Jerome, Motte, Magali, Cooper, Christopher B, Andries, Koen, Van den Broeck, Walter, Franzblau, Scott G, Upton, Anna M, Denny, William A, Palmer, Brian D, Conole, Daniel

“…Bedaquiline (1) is a new drug for tuberculosis and the first of the diarylquinoline class. It demonstrates excellent efficacy against TB but induces…”
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Synthesis and Structure−Activity Relationships of Aza- and Diazabiphenyl Analogues of the Antitubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824) by Kmentova, Iveta, Sutherland, Hamish S, Palmer, Brian D, Blaser, Adrian, Franzblau, Scott G, Wan, Baojie, Wang, Yuehong, Ma, Zhenkun, Denny, William A, Thompson, Andrew M

“…New heterocyclic analogues of the potent biphenyl class derived from antitubercular drug PA-824 were prepared, aiming to improve aqueous solubility but…”
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Synthesis and Structure−activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains by Sutherland, Hamish S, Blaser, Adrian, Kmentova, Iveta, Franzblau, Scott G, Wan, Baojie, Wang, Yuehong, Ma, Zhenkun, Palmer, Brian D, Denny, William A, Thompson, Andrew M

“…Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble…”
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Synthesis and Structure–Activity Relationships of Varied Ether Linker Analogues of the Antitubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824) by Thompson, Andrew M, Sutherland, Hamish S, Palmer, Brian D, Kmentova, Iveta, Blaser, Adrian, Franzblau, Scott G, Wan, Baojie, Wang, Yuehong, Ma, Zhenkun, Denny, William A

“…New analogues of antitubercular drug PA-824 were synthesized, featuring alternative side chain ether linkers of varying size and flexibility, seeking drug…”
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Structure–Activity Relationships for Amide-, Carbamate-, And Urea-Linked Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824) by Blaser, Adrian, Palmer, Brian D, Sutherland, Hamish S, Kmentova, Iveta, Franzblau, Scott G, Wan, Baojie, Wang, Yuehong, Ma, Zhenkun, Thompson, Andrew M, Denny, William A

“…Analogues of clinical tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)­benzyl]­oxy}-6,7-dihydro-5H-imidazo­[2,1-b]­[1,3]­oxazine (PA-824), in which the…”
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Isobenzofurans and ortho-benzoquinone monoketals in syntheses of xestoquinone and its 9- and 10-methoxy derivatives by Sutherland, Hamish S, Higgs, Kerianne C, Taylor, Nicholas J, Rodrigo, Russell

“…Syntheses of (±)-xestoquinone, (±)-9-methoxyxestoquinone and (±)-10-methoxyxestoquinone are described. A convergent CD plus ABE plan using the appropriate…”
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Therapeutic reactivation of mutant p53 protein by quinazoline derivatives by Sutherland, Hamish S., Hwang, In Young, Marshall, Elaine S., Lindsay, Brent S., Denny, William A., Gilchrist, Catherine, Joseph, Wayne R., Greenhalgh, Debra, Richardson, Emma, Kestell, Philip, Ding, Angela, Baguley, Bruce C.

“…Summary Purpose The human tumour suppressor protein p53 is mutated in nearly half of human tumours and most mutant proteins have single amino acid changes…”
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A Two-Step Conversion of α,β-Unsaturated Ketones to Their α-Carbalkoxy or α-Carbamoyl Derivatives by Souza, Fabio E. S, Sutherland, Hamish S, Carlini, Rina, Rodrigo, Russell

“…Several enones are converted into their α-iodo derivatives in excellent yields and carbonylated with palladium catalysis in the presence of alcohol or amines…”
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Insertion reactions of alkenes with diterpenoid chromium aminocarbenes by Woodgate, Paul D, Sutherland, Hamish S

“…Insertion reactions of electron-deficient alkenes with chromium aminocarbenes derived from podocarpic acid generally give aryl ketone products derived from…”
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