1607465-01-9

Upstream product

• 53173-92-5 N-(4-(3'-nitrophenyl)thiazol-2-yl)acetamide 
• 2227-64-7 3'-nitro-2-bromoacetophenone 
• 121-89-1 3-Nitroacetophenone 
• 4530-20-5 BOC-glycine 
• 134812-30-9 N-(4-(3'-aminophenyl)thiazol-2-yl)acetamide 

Downstream Products

• 1607465-10-0 Nα,Nδ-di-tert-butoxycarbonyl[N-(2-N-acetylamino-4-(3-aminophenyl)thiazole)-2-aminoacetamide]histidinamide 
• 1607465-13-3 [N-(2-N-acetylamino-4-(3-aminophenyl)thiazole)-2-aminoacetamide]histidinamide 

Relevant academic research and scientific papers

Preparation method for terpyridine pyridinium complex and application thereof in reverse transcriptase inhibition

The invention belongs to the field of research and development of HIV inhibitors, and discloses a preparation method for a terpyridine pyridinium (II) complex and application thereof in HIV reverse transcriptase inhibition. The structure of a cationic moiety of the terpyridine pyridinium (II) complex is as shown in a formula I. A preparation process for the terpyridine pyridinium (II) complex is optimized, the raw material cost is low, and the reaction time is short. The obtained complex is high in purity and yield and has good water solubility and excellent spectral properties. The terpyridine pyridinium (II) complex has the capability of selective binding to a TAR region on HIV RNA, and can block the reverse transcription process of viral RNA by reverse transcriptase and inhibit the replication of viral RNA. The terpyridine pyridinium (II) complex is a highly affinitive HIV RNA selective binding reagent and a highly active HIV reverse transcriptase inhibitor, and is an HIV drug having a great application potential.

Artificial nucleobase-amino acid conjugates: A new class of TAR RNA binding agents

The human immunodeficiency virus type-1 (HIV-1) Tat protein stimulates transcriptional elongation. Tat is involved in the transcription machinery by binding to the transactivation response region (TAR) RNA stem-loop structure, which is encoded by the 5 leader sequence found in all HIV-1 mRNAs. Herein, we report the rational design, synthesis, and in vitro evaluation of new RNA binding agents that were conceived in order to bind strongly and selectively to the stem-loop structure of TAR RNA and, thus, inhibit the Tat/TAR interaction. We have demonstrated that the conjugation of modified nucleobases, able to interact specifically with an RNA base pair, and various amino acids allows these motifs to bind the target RNA selectively and in a cooperative manner that leads to the inhibition of viral replication in HIV-infected cells. Kissing interaction: The rational design, synthesis, and in vitro evaluation of new RNA binding agents are reported. The conjugation of an artificial nucleobase, which is able to interact specifically with an RNA base pair (Hoogsteen pairing), and various amino acids leads to efficient binding to the target RNA and the inhibition of viral replication in HIV-infected cells .