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Refereed Journals

2015

[180]

Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model.  N.S. Dambuza, P. Smith, A. Evans, J. Norman; D. Taylor, A. Andayi, T. Egan, K. Chibale, L. Wiesner. Malar J 2015 14, 505 

[179] Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A novel anti-mycobacterial class targeting mycobacterial respiration. R. van der Westhuyzen, S. Winks, C. R. Wilson, G. A. Boyle, R. K. Gessner, C. Soares de Melo, D. Taylor, C. de Kock, M.  Njoroge, C. Brunschwig, N. Lawrence, S.P.S. Rao, F. Sirgel, P. van Helden, R. Seldon, A. Moosa, D. F. Warner, L. Arista, U. H. Manjunatha, P. W. Smith, L. J. Street, and K. Chibale*  J. Med. Chem. 2015, 58, 9371−9381 
[178] Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization C. Soares de Melo, T.-S.Feng, R. van der Westhuyzen, R. K. Gessner, L. J. Street, G. L. Morgans, D.  Warner, A. Moosa, K. Naran, N. Lawrence, H. I.M Boshoff, C. E. Barry 3rd, C. J. Harris, R. Gordon and K. Chibale*. Bioorg. Med. Chem. 201523, 7240–7250.
[177] A novel pyrazolopyridine with in vivo activity in Plasmodium berghei and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines. C. Le Manach, T. Paquet, C. Brunschwig, M. Njoroge, Z. Han, D. Gonzalez Cabrera, S. Bashyam, R. Dhinakaran, D. Taylor; J. Reader, M. Botha, A. Churchyard, S. Lauterbach, T. Coetzer, L.-M. Birkholtz, S. Meister, E. Winzeler, D. Waterson, M. Witty, S. Wittlin, M.-B., Jimenez-Diaz, M. Santos Martinez, S. Ferrer, I. Angulo-Barturen, L. Street
and K. Chibale*  J. Med. Chem. 2015, 58, 8713−8722 
[176] Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G. G. Kaur, K. Singh, E. Pavadai, M. Njoroge, M. Espinoza-Moraga, C. De Kock, P. J. Smith, S. Wittlin and K. Chibale*. Med. Chem. Commun., 2015, 6, 2023 - 2028.
[175] Structure Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines. D. G. Cabrera, F. Douelle, C. Le Manach, Z. Han, T. Paquet, D. Taylor, M. Njoroge, N. Lawrence, L. Wiesner, D. Waterson, M. J. Witty, S. Wittlin, L. J. Street and K. Chibale*  J. Med. Chem. 2015, 58, 7572−7579

[174]

Primaquine-pyrimidine hybrids: Synthesis and dual-stage antiplasmodial activity. H. Kaur, M. Machado, C. de Kock, P. Smith, K. Chibale, M. Prudencio and K. Singh. Eur. J. Med. Chem., 2015, 101, 266-273.

[173]

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. H. Kaur, J. Balzarini, C. de Kock, PJ. Smith, K. Chibale and K. Singh. Eur. J. Med. Chem., 2015, 101, 52-62.

[172] Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities. R. Chopra, C. de Kock, P. Smith, K. Chibale and K. Singh. Eur. J. Med. Chem., 2015, 100, 1-9.
[171] Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.  D. S. B. Ongarora, N. Strydom, K. Wicht, M. Njoroge, L.Wiesner, T.J. Egan, S. Wittlin, U. Jurva, C. M. Masimirembwa and K. Chibale*. Bioorg. Med. Chem. 201523 (17), 5419–5432.
[170] Chloroquine-containing compounds: a patent review (2010-2014).  P. Njaria, J. Okombo, N. Njuguna and K. Chibale* Expert Opin. Ther. Patents 2015, 25(9) 1003-1024
[169] Synthesis, antimycobacterial evaluation and pharmacophore modeling of analogues of the natural product formononetin.  P. Mutai, E. Pavadai, I. Wiid, A. Ngwane, B. Baker, and K. Chibale*  Bioorg. Med. Chem. Lett.  2015, 25, 2510-2513.
[168] Crystallisation of an Unexpected Trinuclear Heteronuclear Carbosilane Congener of Ferroquine. Y. Li, K. Chibale, G. S. Smith* J Chem Crystallogr 2015 4, 202–206.

[167]

Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes. M. Adams, C. de Kock, P. J. Smith,K. M. Land, N. Liu, M. Hopper, A. Hsiao, A. R. Burgoyne, T. Stringer, M. Meyer, L. Wiesner, K. Chibale and G. S. Smith* Dalton Trans., 2015, 44, 2456-2468.

[166]

Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antimalarial/antifungal activity. S. Vandekerckhove, S. Van Herreweghe, J. Willems, B. Danneels, T. Desmet, C. de Kock, P. J. Smith, K. Chibale and M. D’hooghe. Eur. J. Med. Chem, 2015, 92, 91-102.

[165]

Synthesis and Structure-Activity-Relationship Studies of Thiazolidinediones as Antiplasmodial Inhibitors of the Plasmodium falciparum Cysteine Protease Falcipain-2. R. K. Sharma, Y. Younis, G. Mugumbate, M. Njoroge, J. Gut, P. J. Rosenthal and K. Chibale*. Eur. J. Med. Chem, 2015, 90, 507-518.