5702-82-9Relevant academic research and scientific papers
Ammonium chloride-catalyzed four-component sonochemical synthesis of novel hexahydroquinolines bearing a sulfonamide moiety
Hussein
, p. 54 - 64 (2015/03/04)
Ammonium chloride as a very inexpensive and readily available reagent efficiently catalyzes one-pot four-component condensation of dimedone with aromatic aldehyde, malononitrile or ethyl cyanoacetate, and sulfonamide derivatives in ethanol at 70°C under ultrasonic irradiation to afford the corresponding 2-amino-4-aryl-1,4,5,6,7,8-hexahydroquinolines bearing a sulfonamide moiety in high yields. In comparison to conventional methods, high yields, easy work-up, and short reaction time are advantages of this sonochemical procedure. The effects of the catalyst, solvent, and temperature are assessed.
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
experimental part, p. 3612 - 3620 (2009/12/09)
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.
Synthesis and antimicrobial evaluation of guanylsulfonamides
Patel, Pratik R.,Ramalingan, Chennan,Park, Yong-Tae
, p. 6610 - 6614 (2008/09/18)
A series of guanylsulfonamides, 2-amino-9-[2-substituted-4-(4-substituted piperidin-1-sulfonyl)phenyl]-1,9-dihydropurin-6-ones, was synthesized by adopting reductive aminoformylation of 2-amino-5-nitro-6-[4-(piperidin-1-sulfonyl)phenylamino]-3H-pyrimidin- 4-one and subsequent intramolecular ring condensation as key steps. All the guanylsulfonamides were assayed for their in vitro antibacterial activities against Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, and Streptococcus faecalis, and their antifungal activities against Aspergillus flavus, Aspergillus niger, and Candida albicans. Of the guanylsulfonamides, 13e and 13f displayed better antibacterial activities than that of Norfloxacin against the bacterial strains S. aureus and S. faecalis except 13f against S. faecalis, which exhibited the activity similar to that of Norfloxacin. Against the fungal strains A. flavus and A. niger, 13g and 13h showed similar activities to that of Griseoflavin-16 except 13h against A. niger, which displayed a profound drop in the activity compared to that of Griseoflavin-16. The remarkable inhibition of the growth of the bacterial and fungal strains makes these substances promising microbial agents.
NOVEL ADENOSINE A3 RECEPTOR AGONISTS
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Page/Page column 27, (2008/06/13)
The invention realizes that a series of sulfonamido derivatives with a conserved uronamide group at the 5' position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido deritatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
