1362020-80-1

Upstream product

• 90-04-0 2-methoxy-phenylamine 
• 623-47-2 propynoic acid ethyl ester 
• 20442-97-1 2-methoxylphenyl azide 

Downstream Products

• 1362020-46-9 (4-(2-chloro-4-nitrophenyl)piperazin-1-yl)(1-(2-methoxyphenyl)-1H-1,2,3-triazol-5-yl)methanone 
• 1267198-33-3 3-(2-methoxyphenyl)-1,2,3-triazole-4-carboxylic acid 

Relevant academic research and scientific papers

THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS

Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

Alkyl Propiolates Participated [3+2] Annulation for the Switchable Synthesis of 1,5- and 1,4-Disubstituted 1,2,3-Triazoles Containing Ester Side Chain

By means of a featured enamine activation, the alkyl propiolates have been successfully employed in the [3+2] annulation for the synthesis of 1,2,3-triazoles. The synthesis of both 1,4- as well as the hardly available 1,5-disubstituted 1,2,3-triazoles can be selectively accessed by using tosyl azide and tosyl hydrazine as nitrogen source, respectively.

Design, synthesis, and in vitro biological evaluation of 1 H -1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents targeting virus nucleoprotein

The influenza virus nucleoprotein (NP) is an emerging target for anti-influenza drug development. Nucleozin (1) and its closely related derivatives had been identified as NP inhibitors displaying anti-influenza activity. Utilizing 1 as a lead molecule, we successfully designed and synthesized a series of 1H-1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents. One of the most potent compounds, 3b, inhibited the replication of various H3N2 and H1N1 influenza A virus strains with IC 50 values ranging from 0.5 to 4.6 μM. Compound 3b also strongly inhibited the replication of H5N1 (RG14), amantidine-resistant A/WSN/33 (H1N1), and oseltamivir-resistant A/WSN/1933 (H1N1, 274Y) virus strains with IC 50 values in sub-μM ranges. Further computational studies and mechanism investigation suggested that 3b might directly target influenza virus A nucleoprotein to inhibit its nuclear accumulation.