88858-84-8Relevant articles and documents
Synthesis and pharmacological evaluation of N-phenyl-acetamide sulfonamides designed as novel non-hepatotoxic analgesic candidates
de Castro Barbosa, Maria Leticia,de Albuquerque Melo, Gabriela Muniz,da Silva, Yolanda Karla Cupertino,de Oliveira Lopes, Raquel,de Souza, Everton Tenorio,de Queiroz, Aline Cavalcanti,Smaniotto, Salete,Alexandre-Moreira, Magna Suzana,Barreiro, Eliezer J.,Lima, Lidia Moreira
, p. 3612 - 3620 (2009)
In this paper we report the design, synthesis and pharmacological evaluation of a series of N-phenyl-acetamide sulfonamide derivatives (5a-g), planned by structural modification on the prototype paracetamol (1). In this series (5a-g), compound LASSBio-1300 (5e; ID50 = 5.81 μmol/kg) stands out as a new non-hepatotoxic analgesic drug candidate. The increase of area, volume and eletrostatic potential of paracetamol's analogues seems to be beneficial to the analgesic activity. Unlike paracetamol (1) and the other analogues (5a, 5d-g), compounds 5b and 5c presented an important anti-hypernociceptive activity associated to inflammatory pain.
Adenosine A3 receptor modulators
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, (2008/06/13)
The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceu
SUBSTITUTED CINNAMIC, ACID GUANIDIDES, PROCESS FOR THEIR PREPARATION, THEIR USE AS A MEDICAMENT, AND MEDICAMENT COMPRISING THEM
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, (2008/06/13)
Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the 1, which may be obtained by reaction of a compound II 2with guanidine.
