81933-79-1Relevant academic research and scientific papers
Synthesis of New Heterocycles from Reactions of 1-Phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonyl Azides
Aly, Ashraf A.,El-Emary, Talaat I.,Mourad, Aboul-Fetouh E.,Alyan, Zainab Khallaf,Br?se, Stefan,Nieger, Martin
, p. 1369 - 1375 (2019/02/19)
Two individual examples of pyrazolo[3,4-b]pyridine-5-carbonyl azides and hydrazides were reacted with various nucleophilic reagents. Different unexpected behaviors was observed. NMR, IR, mass spectra together with elemental analyses and X-ray structure analyses, were used to prove the structure of the obtained products.
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity
Panda, Manoranjan,Ramachandran, Sreekanth,Ramachandran, Vasanthi,Shirude, Pravin S.,Humnabadkar, Vaishali,Nagalapur, Kavitha,Sharma, Sreevalli,Kaur, Parvinder,Guptha, Supreeth,Narayan, Ashwini,Mahadevaswamy, Jyothi,Ambady, Anisha,Hegde, Naina,Rudrapatna, Suresh S.,Hosagrahara, Vinayak P.,Sambandamurthy, Vasan K.,Raichurkar, Anandkumar
supporting information, p. 4761 - 4771 (2014/07/07)
A novel pyrazolopyridone class of inhibitors was identified from whole cell screening against Mycobacterium tuberculosis (Mtb). The series exhibits excellent bactericidality in vitro, resulting in a 4 log reduction in colony forming units following compound exposure. The significant modulation of minimum inhibitory concentration (MIC) against a Mtb strain overexpressing the Rv3790 gene suggested the target of pyrazolopyridones to be decaprenylphosphoryl- β-d-ribose-2′-epimerase (DprE1). Genetic mapping of resistance mutation coupled with potent enzyme inhibition activity confirmed the molecular target. Detailed biochemical characterization revealed the series to be a noncovalent inhibitor of DprE1. Docking studies at the active site suggest that the series can be further diversified to improve the physicochemical properties without compromising the antimycobacterial activity. The pyrazolopyridone class of inhibitors offers an attractive non-nitro lead series targeting the essential and vulnerable DprE1 enzyme for the discovery of novel antimycobacterial agents to treat both drug susceptible and drug resistant strains of Mtb.
A facile synthesis of pyrazolo[3,4-b]pyridines
Ahluwalia,Goyal, Bindu
, p. 1341 - 1348 (2007/10/03)
Pyrazolo[3,4-b]pyridines (4) and (5) have been obtained by the condensation of 3-(alkyl/aryl)-5-amino-1-phenyl-1H-pyrazole-4-carboxaldehydes (3) with active methylene compounds viz: diethyl malonate and malononitrile.
AMINOPYRAZOLES, II; SYNTHESIS OF PYRAZOLOPYRIDINES VIA VILSMEIER-HAACK REACTION OF 5-ACETAMINOPYRAZOLES
Simay, A.,Takacs, K.,Toth, L.
, p. 175 - 188 (2007/10/02)
The title compounds 4 and 5 were isolated as by-product in the Vilsmeier-Haack reaction of 5-acetylaminopyrazoles 1.The structures were supported spectroscopically and proved by a preparative route.On the basis of preliminary investigation of the mechanis
