101875-03-0Relevant articles and documents
Some studies in sulfadiazine incorporating pyridine, pyrimidine, oxadiazole, and azo moieties endowed with pharmaceutical potency
Abu-Melhab, Sraa,El-Hadidya, Sherihan A.
, p. 167 - 178 (2020/03/30)
A set of substituted sulfadiazine compounds was prepared as cytotoxic and antitumor agents by using 4-amino-N-(py-rimidin-2-yl)benzenesulfonamide (1) as the starting material. Compound 1 was reacted with different reagents to give the corresponding sulfadiazines 2-18 and hydrozaones 19a-h which were evaluated for their in vitro cytotoxicity versus four cancer cell lines. Compounds 3, 5, 19d and 19h were active against the tested cancer cells.
Synthesis and evaluation of novel dapsone-thalidomide hybrids for the treatment of type 2 leprosy reactions
Yamasaki, Paulo Renato,Do Nascimento, Dejair Caetano,Chelucci, Rafael Consolin,De Faria Fernandes Belone, Andréa,Rosa, Patrícia Sammarco,Diório, Suzana Madeira,De Melo, Thais Regina Ferreira,Barbieri, Karina Pereira,Placeres, Marisa Campos Polési,Carlos, Iracilda Zepone,Chung, Man Chin,Dos Santos, Jean Leandro
, p. 3084 - 3087 (2014/06/24)
We synthesized a series of novel dapsone-thalidomide hybrids (3a-i) by molecular hybridization and evaluated their potential for the treatment of type 2 leprosy reactions. All of the compounds had analgesic properties. Compounds 3c and 3h were the most active antinociceptive compounds and reduced acetic acid-induced abdominal constrictions by 49.8% and 39.1%, respectively. The hybrid compounds also reduced tumor necrosis factor-α levels in lipopolysaccharide-stimulated L929 cells. Compound 3i was the most active compound; at concentrations of 15.62 and 125 μM, compound 3i decreased tumor necrosis factor-α levels by 86.33% and 87.80%, respectively. In nude mice infected with Mycobacterium leprae in vivo, compound 3i did not reduce the number of bacilli compared with controls. Compound 3i did not have mutagenic effects in Salmonella typhimurium strains TA100 and TA102, with or without metabolic activation (S9 mixture). Our results indicate that compound 3i is a novel lead compound for the treatment of type 2 leprosy reactions.
Synthesis and evaluation of novel dapsone-thalidomide hybrids for the treatment of type 2 leprosy reactions
Yamasaki, Paulo Renato,Do Nascimento, Dejair Caetano,Chelucci, Rafael Consolin,De Faria Fernandes Belone, Andra,Rosa, Patrcia Sammarco,Dirio, Suzana Madeira,De Melo, Thais Regina Ferreira,Barbieri, Karina Pereira,Placeres, Marisa Campos Polsi,Carlos, Iracilda Zepone,Chung, Man Chin,Dos Santos, Jean Leandro
, p. 3084 - 3087 (2015/02/19)
We synthesized a series of novel dapsone-thalidomide hybrids (3a-i) by molecular hybridization and evaluated their potential for the treatment of type 2 leprosy reactions. All of the compounds had analgesic properties. Compounds 3c and 3h were the most active antinociceptive compounds and reduced acetic acid-induced abdominal constrictions by 49.8% and 39.1%, respectively. The hybrid compounds also reduced tumor necrosis factor-α levels in lipopolysaccharide-stimulated L929 cells. Compound 3i was the most active compound; at concentrations of 15.62 and 125 μM, compound 3i decreased tumor necrosis factor-α levels by 86.33% and 87.80%, respectively. In nude mice infected with Mycobacterium leprae in vivo, compound 3i did not reduce the number of bacilli compared with controls. Compound 3i did not have mutagenic effects in Salmonella typhimurium strains TA100 and TA102, with or without metabolic activation (S9 mixture). Our results indicate that compound 3i is a novel lead compound for the treatment of type 2 leprosy reactions.
Synthesis and in vitro anti Mycobacterium tuberculosis activity of a series of phthalimide derivatives
Santos, Jean L.,Yamasaki, Paulo R.,Chin, Chung Man,Takashi, Celio H.,Pavan, Fernando R.,Leite, Clarice Q.F.
experimental part, p. 3795 - 3799 (2009/09/30)
New phthalimide derivatives were easily prepared through condensation of phthalic anhydride and selected amines with variable yields (70-90%). All compounds (3a-l) were evaluated against Mycobacterium tuberculosis H37Rv using Alamar Blue susceptibility. The compounds 3c, 3i, and 3l have the minimum inhibitory concentrations (MICs) of 3.9, 7.8, and 5.0 μg/mL, respectively, and could be considered new lead compounds in the treatment of tuberculosis and multi-drug resistant tuberculosis. Crown Copyright
