Search

Papers in refereed journals

2014

[164]

Recent Approaches to Chemical Discovery and Development Against Malaria and the Neglected Tropical Diseases Human African Trypanosomiasis and Schistosomiasis. M. Njoroge, N. Njuguna, P. Mutai, D. Ongarora, P. Smith, and K. Chibale*. Chem. Rev. 2014, 114, 11138−11163.

[163] Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2.  C. Le Manach, T. Paquet, D. Gonzalez Cabrera, Y. Younis, D. Taylor, L. Wiesner, N. Lawrence, S. Schwager, D. Waterson, M. J. Witty, S. Wittlin, L. Street, and K. Chibale*. J. Med. Chem. 2014, 57, 8839−8848.

[162]

Structure-activity relationship studies of antiplasmodial aminomethylthiazoles. P. M. Cheuka, D. G. Cabrera, T. Paquet and K. Chibale*. Bioorg. Med. Chem. Lett. 2014, 24, 5207-5211.

[161]

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity. R. Thelingwani,* B. Bonn, K. Chibale, C.M. Masimirembwa. Expert Opin Drug Metab Toxicol. 2014, 10(10), 1313-1324.

[160]

Synthesis and Evaluation of a Carbosilane Congener of Ferroquine and Its Corresponding Heterometallic Organometallic Complexes for Antiplasmodial and -Hematin Inhibition Activity. Y. Li, C. de Kock, P. J. Smith, K. Chibale,* and G. S. Smith.* Organometallics 2014, 33, 4345−4348.

[159]

Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery. E.M. Kigondu, A. Wasuna, D.F. Warner*, and K. Chibale*. Bioorg. Med. Chem. 2014, 22, 4453-4461.

[158]

Kojic acid derived hydroxypyridinone-chloroquine hybrids: Synthesis, crystal structure, antiplasmodial activity and -haematin inhibition W. A. Andayi, T. J. Egan and K. Chibale* Bioorg. Med. Chem. Lett. 2014, 24, 3263-3267.

[157]

Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c. K. Singh, M. Kumar, E. Pavadai, K. Naran, D. F. Warner, P. G. Ruminski and K. Chibale* Bioorg. Med. Chem. Lett. 2014, 24, 2985-2990.

[156] Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1.  C. Le Manach, D. Gonzalez Cabrera, F. Douelle, A. T. Nchinda, Y. Younis, D. Taylor, L. Wiesner, K. White, E. Ryan, C. March, S. Duffy, V. Avery, D. Waterson, M. J. Witty, S. Wittlin; S. Charman, L. Street, and K. Chibale*. J. Med. Chem. 2014, 57, 2789-2798.

[155]

Effects of a domain-selective ACE inhibitor in a mouse model of chronic angiotensin II-dependent Hypertension. D. Burger, T.L. Reudelhuber, A. Mahajan, K. Chibale, E.D. Sturrock, and R.M. Touyz*. Clinical Science 2014, 127, 57-63.

[154]

Pharmacokinetic evaluation of lisinopril-tryptophan, a novel C-domain ACE inhibitor. P. Denti, S.-K. Sharp, W.L. Kröger, S. L. Schwager, A. Mahajan, M. Njoroge, L. Gibhard, I. Smit, K. Chibale, L. Wiesner, E. D. Sturrock*, N. Davies. European Journal of Pharmaceutical Sciences 2014, 56, 113-119 .

[153]

Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects. D.L. Cruickshank, Y.Younis, N.M. Njuguna, D.S. B. Ongarora, K. Chibale and Mino R. Caira* CrystEngComm. 2014, 16, 5781-5792.

[152]

Synthesis and medicinal chemistry of selected antitubercular natural products and natural product derivatives. A. Mahajan, R. Hans, K. Chibale, V.Kumar,* RSC Adv., 2014, 4, 15180-15215.

[151]

Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites. E.M. Kigondu, M. Njoroge, K. Singh, N. Njuguna, D. F. Warner, and K. Chibale*. Med. Chem. Commun., 2014, 5, 502-506.

[150] 2,4-Diamino-thienopyrimidines as Orally Active Antimalarial Agents. D. G. Cabrera, C. Le Manach, F. Douelle, Y. Younis, T.-S. Feng, T. Paquet, A.T. Nchinda, L. J. Street, D. Taylor, C. de Kock, L. Wiesner, S. Duffy, K.L. White, K.M. Zabiulla, Y. Sambandan, S. Bashyam, D. Waterson, M.J. Witty,  S.A. Charman, V.M. Avery, S. Wittlin, and K. Chibale*. J. Med. Chem. 2014, 57, 1014-1022.

[149]

Quinoline-pyrimidine hybrids: Synthesis, antiplasmodial activity, SAR and mode of action studies. K. Singh*, H. Kaur; P. J. Smith, C. de Kock, K. Chibale, J. Balzarini. J. Med. Chem. 2014, 57, 435−448.

[148]

The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice. E. T. Abay, J.H. van der Westuizen, K.J. Swart, L. Gibhard, M. Tukulula , K. Chibale, L. Wiesner*. Malaria Journal 2014, 13, 42.

[147]

Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity. S. Vandekerckhove, T. Desmet, H. G. Tran, C. de Kock, P.J. Smith, K. Chibale and M. D’hooghe* Bioorg. Med. Chem. Lett. 2014, 24, 1214-1217.

[146]

Synthesis of Metergoline analogues and their evaluation as antiplasmodial agents. K. Singh, G. Kaur, F. Mjambili, P. J. Smith and K. Chibale*. Med. Chem. Commun., 2014, 5 (2), 165 - 170.

[145]

Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents. F. Mjambili, M. Njoroge, K. Naran, C. De Kock, P.J. Smith, V. Mizrahi, D. Warner, and K. Chibale*. Bioorg. Med. Chem. Lett. 2014, 24, 560-564.

[144]

Synthesis and evaluation of new polynuclear organometallic Ru(II), Rh(III) and Ir(III) pyridyl ester complexes as in vitro antiparasitic and antitumor agents. P. Chellan, K.M. Land, A.Shokar, A. Au, S. H. An, D. Taylor, P. J. Smith,T. Riedel, P. J. Dyson, K. Chibale and G. S. Smith* Dalton Trans., 2014, 43(2), 513 - 526.

[143]

Fragment-based design for the development of N-domain-selective angiotensin-1-converting enzyme inhibitors. R.G. Douglas, R.K. Sharma, G. Masuyer, L. Lubbe, I. Zamora, K.R. Acharya*, K. Chibale* and E.D Sturrock* Clinical Science 2014, 126, 305−313.