1610875-95-0

Upstream product

• 139756-01-7 1-methyl-4-nitro-3-propyl-1H-pyrazole-5-carboxamide 
• 139756-00-6 1-methyl-2-nitro-3-propyl-1H-pyrazole-5-carboxylic acid 
• 139755-99-0 1-methyl-3-propyl-1 H-pyrazole-5-carboxylic acid 
• 133261-07-1 1-Methyl-3-n-propylpyrazole-5-carboxylic acid ethyl ester 
• 92945-27-2 ethyl 3-propyl-1H-pyrazole-5-carboxylate 
• 351-54-2 3-fluoro-p-anisaldehyde 
• 139756-02-8 4-amino-1-methyl-3-propyl-1H-pyrazole-5-carboxamide 

Relevant academic research and scientific papers

Synthesis of 5-substituted-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one analogs and their biological evaluation as anticancer agents: mTOR inhibitors

A microwave assisted strategy for synthesis of series of 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones has been developed and their biological evaluation as anticancer agents is described. The synthetic protocol involves simple procedure by oxidative coupling of 4-amino-1-methyl-3-propyl-1H-pyrazole- 5-carboxamide with different aldehydes in presence of K2S 2O8 offering 5-substituted-1H-pyrazolo[4,3-d]pyrimidin- 7(6H)-one compounds in excellent yields. The in vitro anticancer activity screening against human cancer cell lines HeLa, CAKI-I, PC-3, MiaPaca-2, A549 gave good results. The in detailed mechanistic correlation studies of compound 3m revealed that the compound shows anticancer activity through apoptosis mechanism and also inhibits mTOR with nonomolar potency. The design was based on docking with mTOR protein. The concentration dependent cell cycle analysis, western blotting experiment and nuclear cell morphology studies have been described.

PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF IMPOTENCE AND PROCESS FOR THE PREPARATION THEREOF

The present invention relates to Pyrazolopyrimidinone compounds as PDE5 inhibitors with better IC50 value, good in vivo efficacy and PK profile and a process for the preparation thereof. The present invention covers the pyrazolo pyrimidinone based compounds that have been designed, synthesized and screened for PDE5 inhibitory activity and its PDE5 inhibitory potential is provided in this invention. These designer compounds have shown nanomolar potency when screened for PDE5 inhibitory activity and also shown better in vivo efficacy. These compounds can be used in the treatment of male erectile dysfunction or in the treatment of impotence.