Article, Ajoutée
le 17/01/2017 10:11
In a drug discovery program aimed at finding new anti-trypanosomal drugs, we developed the N, Ndimethylformamide.diiodine complex (DMF.I2) as an innovative and efficient green catalyst for the condensation reaction of aldehydes/ketones with arylthios [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI FERNAND A. [2],
MCCURDY CHRISTOPHER R. [3],
POUPAERT JACQUES H. [4],
Article, Ajoutée
le 17/01/2017 10:25
Relying on a straightforward « Green-Chemistry » based approach, this article reports an optimized Diels-Alder (DA) experimental set-up allowing for this reaction to be cleanly operated in the presence of water used both as solvent and catalyst. Thi [...]
GBAGUIDI A. FERNAND [1],
KASSÉHIN URBAIN C. [2],
PREVOST JULIEN R. C. [3],
FREDERICK RAPHAËL [4],
MCCURDY CHRISTOPHER R. [5],
POUPAERT JACQUES H. [6],
Article, Ajoutée
le 17/01/2017 10:32
Agomelatine, a melatonin-like antidepressant drug based on a naphthalene scaffold, has received considerable attention these last twenty years. This drug molecule undergoes important liver first pass effect and suffers therefore of a short plasma hal [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
MCCURDY CHRISTOPHER R. [3],
POUPAERT JACQUES H. [4],
Article, Ajoutée
le 17/01/2017 10:54
African trypanosomiasis remains a life-threatening disease and there is nowadays an urgent need for improved therapeutic agents for this pathology. In this context, in order to create novel anti-protozoa prototype containing both a trypanocidal thios [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
MCCURDY CHRISTOPHER R. [3],
POUPAERT JACQUES H. [4],
Article, Ajoutée
le 17/01/2017 11:37
Trypanosomiasis constitutes a severe health problem for sub-saharian African and latin American population and there is an urgent need for better drugs to cure this life-threatening disease. In this context, aromatic thiosemicarbazones appears attrac [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
MCCURDY CHRISTOPHER R. [3],
POUPAERT JACQUES H. [4],
Article, Ajoutée
le 17/01/2017 11:52
[...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
KAPANDA COCO N. [3],
MCCURDY CHRISTOPHER R. [4],
POUPAERT JACQUES H. [5],
Article, Ajoutée
le 18/01/2017 09:01
Based on a rational approach using merely bioisosterism as euristic tool, we designed and tested a short series of congeners of 6-benzoyl-2(3H)-benzoxazolone as phenytoinergic lead. Among them, 5-benzoyloxindole showed an impressive activity in the M [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
CARATO PASCAL [3],
MCCURDY CHRISTOPHER R. [4],
POUPAERT JACQUES H. [5],
Article, Ajoutée
le 18/01/2017 10:44
A concise series of aldehydes and ketones were reacted in a condensation reaction with 4phenylthiosemicarbazide in order to assess the relative influence of the steric and electronic effects in the control of this reaction. While steric effects had a [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
KAPANDA COCO N. [3],
MCCURDY CHRISTOPHER R. [4],
BIGOT ANDRÉ K. [5],
POUPAERT JACQUES H. [6],
Article, Ajoutée
le 19/01/2017 10:29
Based on a line of evidence (logP, pKa, 1H-, and 13C-NMR, and molecular modeling studies), it appears that cocaine undergoes a hydrophobic collapse which may account for its unprecedented ADME properties, in particular, its exceptional capacity to cr [...]
POUPAERT JACQUES H. [1],
GBAGUIDI A. FERNAND [2],
KAPANDA COCO N. [3],
AICHAOUI HOCINE [4],
MCCURDY CHRISTOPHER R. [5],
Article, Ajoutée
le 25/01/2017 08:29
A green synthesis of tetracyclone (2, 3, 4, 5-tetraphenyl-2, 4-cyclopentadien-1-one) has been conceived and executed on the basis of a rationale design. Three separate, “green” processes to synthesize tetracyclone were undertaken to compare homogeneo [...]
KASSÉHIN URBAIN C. [1],
GBAGUIDI A. FERNAND [2],
CARATO PASCAL [3],
MCCURDY CHRISTOPHER R. [4],
ACCROMBESSI GEORGES C. [5],
POUPAERT JACQUES H. [6],