2199-63-5Relevant articles and documents
Synthesis, structure and in vitro anti-trypanosomal activity of non-toxic arylpyrrole-based chalcone derivatives
Hoppe, Heinrich C.,Isaacs, Michelle,Khanye, Setshaba D.,Kruger, Cuan,Oderinlo, Ogunyemi O.,Smith, Vincent J.,Veale, Clinton G. L.,Zulu, Ayanda I.
supporting information, (2020/04/10)
With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC50 values of 4.09 and 5.11 μM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.
Versatility of Weinreb amides in the Knorr pyrrole synthesis
Alberola, Angel,Ortega, Alfonso Gonzalez,Sadaba, M. Luisa,Sanudo, Carmen
, p. 6555 - 6566 (2007/10/03)
N-Methoxy-N-methyl-α-enaminocarboxamides were prepared starting from enamines and Weinreb α-aminoamides. Their reaction with oganometallic compounds and subsequent cyclization constitute a versatile alternative in the Knorr pyrrole synthesis.
SYNTHESE DE PYRROLES ET D'OXAZOLES PAR PYROLYSE DE N-(HYDROXY-2' ETHYL) AMINO-3 PROPENOATE
Pale-Grosdemange, Catherine,Chuche, Josselin
, p. 3397 - 3414 (2007/10/02)
The gas phas pyrolysis of various N-(2'-hydroxyethyl)-3-amino propenoates 1-6 and N-(2'-hydroxy-2'-phenyl ethyl)-3-amino propanoate 7-9 at 390 deg C-420 deg C leads respectively to formylpyrroles 11-16 and benzoylpyrroles 17-19 and, in some cases, to substituted oxazoles 36-39.The results are best explained by the intermediate formation of a dicarbonyl derivative followed either by an intramolecular thermal crotonisation or a six ? electrocyclization of an azomethine ylide.