1203605-01-9

Upstream product

• 1203605-56-4 tert-butyl [2-(2-{[5-(4-amino-2,6-dimethyl-phenyl)-[1,2,4]triazin-3-ylamino]-methyl}-benzothiazol-5-yloxy)-ethyl]-carbamate 
• 1203605-55-3 tert-butyl [4-(3-{[5-(2-tert-butoxycarbonylaminoethoxy)benzothiazol-2-ylmethyl]amino}[1,2,4]triazin-5-yl)-3,5-dimethylphenyl]carbamate 
• 1203605-54-2 [2-(2-aminomethylbenzothiazol-5-yloxy)ethyl]carbamic acid tert-butyl ester 
• 1203605-57-5 {2-[2-({5-[4-(2-dimethylaminoethylamino)-2,6-dimethylphenyl][1,2,4]triazin-3-ylamino}methyl)benzothiazol-5-yloxy]ethyl}carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Vectorization efforts to increase Gram-negative intracellular drug concentration: A case study on HldE-K inhibitors

In this paper, we present different strategies to vectorize HldE kinase inhibitors with the goal to improve their Gram-negative intracellular concentration. Syntheses and biological effects of siderophoric, aminoglycosidic, amphoteric, and polycationic vectors are discussed. While siderophoric and amphoteric vectorization efforts proved to be disappointing in this series, aminoglycosidic and polycationic vectors were able for the first time to achieve synergistic effects of our inhibitors with erythromycin. Although these effects proved to be nonspecific, this study provides information about the required stereoelectronic arrangement of the polycationic amines and their basicity requirements to fulfill outer membrane destabilization resulting in better erythromycin synergies.

New 1,2,4-triazine derivatives and biological applications thereof

The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.