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Synthesis and pharmacological evaluation of N-phenyl-acetamide sulfonamides designed as novel non-hepatotoxic analgesic candidates

2009; Elsevier BV; Volume: 44; Issue: 9 Linguagem: Inglês

10.1016/j.ejmech.2009.02.026

1768-3254

Maria Letícia de Castro Barbosa, Gabriela Muniz de Albuquerque Melo, Yolanda Karla Cupertino da Silva, Raquel de Oliveira Lopes, Éverton Tenório de Souza, Aline Cavalcanti de Queiroz, Salete Smaniotto, Magna Suzana Alexandre‐Moreira, Eliezer J. Barreiro, Lı́dia Moreira Lima,

Drug-Induced Hepatotoxicity and Protection

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.