TY  - JOUR
T1  - Design and Synthesis of Functionalized 2,4-Diamino-1,3,5-Triazines, Potential Inhibitors Involved in Immune and Inflammatory Response
A1  - Amelanh Sica Diakité
A1  - Christelle N’ta Mélissa Ambeu-Loko
A1  - Ange Désiré Yapi
A1  - Cédric Logé
A1  - Alain Kacou
A1  - Stéphanie Kra
A1  - Blandine Baratte
A1  - Stéphane Bach
A1  - Sandrine Ruchaud
A1  - Drissa Sissouma
A1  - Mahama Ouattara
A1  - Jean-michel Robert
JF  - International Journal of Pharmaceutical Research and Allied Sciences
JO  - Int J Pharm Res Allied Sci
SN  - 2277-3657
Y1  - 2024
VL  - 13
IS  - 4
DO  - 10.51847/hsT2C61XWx
SP  - 1
EP  - 11
N2  - A two-step synthesis method, initially using a microwave reactor for the preparation of reaction intermediates, allowed us to synthesize eleven 6-aryl-2,4-diamino-1,3,5-triazines 5a-k. The intermediates were biguanide derivatives 3a-f which were synthesized under microwave irradiation for 10 min at 130°C. The 2,4-diamino-1,3,5-triazine derivatives (5a-k) were obtained with yields from 16% to 86%. The compounds synthesized were submitted to biological evaluation on twelve protein kinases, through the implementation of a dose-response method which allowed the determination of median inhibitory concentration or IC50. Indeed, enzymatic activities were carried out in the presence of 10 µM of ATP, in a final volume of 6 µl for 30 min at 30°C in ADP-Glo buffer. Among the triazines synthesized, results of enzymatic activity showed that the most active molecule was compound 5b which inhibited PIM1 kinase with IC50 = 1.18 µg/mL This result is the starting point of a larger research program for our group which could investigate the introduction of the substituted group on triazine’s terminal amino group. 
UR  - https://ijpras.com/article/design-and-synthesis-of-functionalized-24-diamino-135-triazines-potential-inhibitors-involved-in-rzlvm4virwdz5b7
ER  -