294885-56-6Relevant academic research and scientific papers
Effect of photodynamic antibacterial chemotherapy combined with antibiotics on Gram-positive and gram-negative bacteria
Ilizirov, Yana,Formanovsky, Andrei,Mikhura, Irina,Paitan, Yossi,Nakonechny, Faina,Nisnevitch, Marina
, (2018/12/11)
The well-known and rapidly growing phenomenon of bacterial resistance to antibiotics is caused by uncontrolled, excessive and inappropriate use of antibiotics. One of alternatives to antibiotics is Photodynamic Antibacterial Chemotherapy (PACT). In the present study, the effect of PACT using a photosensitizer Rose Bengal alone and in combination with antibiotics including methicillin and derivatives of sulfanilamide synthesized by us was tested against antibiotic-sensitive and antibiotic-resistant clinical isolates of Gram-positive S. aureus and Gram-negative P. aeruginosa. Antibiotic-sensitive and resistant strains of P. aeruginosa were eradicated by Rose Bengal under illumination and by sulfanilamide but were not inhibited by new sulfanilamide derivatives. No increase in sensitivity of P. aeruginosa cells to sulfanilamide was observed upon a combination of Rose Bengal and sulfanilamide under illumination. All tested S. aureus strains (MSSA and MRSA) were effectively inhibited by PACT. When treated with sub-MIC concentrations of Rose Bengal under illumination, the minimum inhibitory concentrations (MIC) of methicillin decreased significantly for MSSA and MRSA strains. In some cases, antibiotic sensitivity of resistant strains can be restored by combining antibiotics with PACT.
USP30 INHIBITORS
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Page/Page column 22, (2018/12/13)
The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
NOVEL ADENOSINE A3 RECEPTOR AGONISTS
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Page/Page column 29, (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.
METHOD OF PREPARING 4-(IMIDAZOLE-1-IL)BENZENESULPHONAMIDE DERIVATIVES
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Page 9, (2008/06/13)
Process for the preparation of 4-(imidazol-1-yl)benzenesulfonamide derivatives of formula I, wherein R1 represents optionally substituted aryl or heteroaryl, which comprises treating a compound of formula II, wherein R1 has the same
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-Diarylimidazoles
Almansa, Carmen,Alfón, José,De Arriba, Alberto F.,Cavalcanti, Fernando L.,Escamilla, Ignasi,Gómez, Luis A.,Miralles, Agustí,Soliva, Robert,Bartrolí, Javier,Carceller, Elena,Merlos, Manuel,García-Rafanell, Julián
, p. 3463 - 3475 (2007/10/03)
The synthesis and the pharmacological activity of a series of 1,5-diarylimidazoles developed as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema, air-pouch, and hyperalgesia tests). Modification of all the positions of two regioisomeric imidazole cores led to the identification of 4-[4-chloro-5-(3-fluoro4-methoxyphenyl)imidazol-1-yl]benzenesulfonamide (UR-8880, 51f) as the best candidate, which is now undergoing Phase I clinical trials.
Synthesis of n-mono-and n,n-disubstituted 4-aminobenzenesulfonamides
Mikhura,Formanovskii
, p. 64 - 68 (2007/10/03)
-N-Mono-and N,N-disubstituted 4-aminobenzenesulfonamides were synthesized by reaction of 4-acetylacetylaminobenzenesulfonyl chloride with the corresponding primary and secondary aliphatic and aromatic amines, followed by removal of the acetyl group via acid hydrolysis.
