Synthesis and Biological Evaluation of Novel Thiazole Hydrazines as Antimicrobial and Antimalarial Agents
Vishnu Gore, Sunil U. Tekale, Someshwar Bhale, Dhanaji P. Rajani, Abraham J. Domb, Rajendra P. Pawar, S Nayak, S Gaonkar, A Rouf, C Tanyeli, S Kashyap, V Garg, P Sharma, N Kumar, R Dudhe, J Gupta, K Alomar, A Landreau, M Kempf, M Khan, M Allain, G Bouet, D Bloom, D Cadarette, J Bedford, J Farrar, C Ihekweazu, G Kang, M Koopmans, J Nkengasong, M Khan, S Xu, M Ali, R Ali, A Kazmi, N Akhtar, M Bilal, Y Hu, F Li, T Parish, A Saleh, M Elnakib, D Malek, M Arop, T Morsy, C Fleischmann-Struzek, D Goldfarb, P Schlattmann, L Schlapbach, K Reinhart, N Kissoon, M Desai, F Ter Kuile, F Nosten, R Mcgready, K Asamoa, B Brabin, R Newman, S Kauthale, S Tekale, M Damale, J Sangshetti, R Pawar, S Kauthale, S Tekale, A Rode, R Patil, J Sangshetti, L Ktai, R Pawar, D Stalons, C Thornsberry, K Rieckmann, L Sax, G Campbell, J Mrema
Abstract
Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against - S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.