Synthesis of Novel -1, 3, 5 - Triazine - Based - Anti-Tuberculosis Drugs.

• Main Author: Rapudi, Munaka
• Other Authors: Moleele, S. Mnyakeni
• Format: Others
• Language: en
• Published: 2018
• Subjects: Synthesis; Drugs; Novel; Triazine; Tuberculosis; 616.995; Tuberculosis > Prevention; Tuberculosis > Vaccination; Triazines; Communicable diseases infection; Terbtryn; Tuberculosis vaccines
• Online Access: Rapudi, Munaka (2018) Synthesis of Novel -1, 3, 5 - Triazine - Based - Anti-Tuberculosis Drugs, University of Venda, Thohoyandou, South Africa, <http://hdl.handle.net/11602/1231>; http://hdl.handle.net/11602/1231

MSc (Chemistry) === Department of Chemistry === Identification of unique leads represents a significant challenge in drug discovery. This challenge is widely visible in neglected diseases such as tuberculosis, which is an infectious disease caused by bacillus Mycobacterium tuberculosis. The urgent need in search of new biological entities to fight back TB and drug resistant TB is a drive behind this project. Several specific synthetic protocols have been developed using 1,3,5-triazines due to the important biological properties which they display. The chemistry and an extensive spectrum of biological activities of s-triazines have been examined since several decades and this heterocyclic core has received emerging consensus. Hence, the aim of this project was to synthesize novel anti-TB drugs total with the usage of 1,3,5-triazine as a linker between known anti-TB drugs together with different types of amines. A total of 20 compounds were synthesized, 3 compounds were mono-substituted with an average yield of 75 %, 6 compounds were di-substituted with an average yield of 63 % and 11 compounds were tri-substituted with an average yield of 93 %. Out of 10 compounds which were analysed for biological activity 8 of which showed biological activity against M.smegmatis. Furthermore compound 26 which was hybridized with an amine and a known anti-TB drug inhibited better biological activity. In conclusion the influence of cyanuric chloride in combination with pyrrolidine and anti-TB drugs deserves further study. The newly synthesized compounds were characterized by IR, melting point, GC-MS, biological testing, 1H and 13C NMR. === NRF