29182-92-1Relevant articles and documents
New N-4 piperazinyl derivatives of norfloxacin: design, synthesis, and correlation of calculated physicochemical parameters with antibacterial activity
Abuo-Rahma, Gamal El-Din,Abbas, Samar,Shoman, Mai,Samir, Ebtihal,Abdel-Baky, Rehab
, p. 1072 - 1085 (2018)
A group of N?4 piperazinyl derivatives of norfloxacin was synthesized and identified by different spectroscopic techniques. The N?4 piperazinyl substituent in target compounds 2a–2k, 3a–3c, and 4a and 4b was designed to have different electronic, steric,
Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities
Elbadawi, Mostafa M.,Eldehna, Wagdy M.,Nocentini, Alessio,Abo-Ashour, Mahmoud F.,Elkaeed, Eslam B.,Abdelgawad, Mohamed A.,Alharbi, Khalid S.,Abdel-Aziz, Hatem A.,Supuran, Claudiu T.,Gratteri, Paola,Al-Sanea, Mohammad M.
, (2021/03/30)
As a front-runner selective CA IX inhibitor currently in Phase Ib/II clinical trials, SLC-0111 has been herein exploited as a lead molecule for development of new different sets of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides incorporating different functionalities; primary sulfonamide (5a-f), free carboxylic (8a, 8d), ethyl ester (8b, 8e), acetyl (8c, 8f) and nitro (10a, 10b), as potential carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. All the prepared analogues have been examined for their CA inhibitory activities towards four human (h) isoenzymes, hCA I, II, IX and XII. Interestingly, replacement of SLC-0111 ureido linker with the flexible sulfonyl acetamide linker, as well as linker branching and elongation strategies successfully enhanced the inhibitory action toward hCA IX isoform, such as in sulfones 5a-d and 5f which displayed better activity than SLC-0111. Furthermore, sulfonamide-based sulfone (5f) and carboxylic acid-based sulfones (8a and 8d) demonstrated interesting selectivity toward the tumor-related hCA IX isoform over both hCA I and hCA II, which suggests them as promising candidates for further development as potential anticancer candidates. Thereafter, the anti-proliferative action for sulfones 5f, 8a and 8d was examined against breast (MCF-7) and colon (HCT-116) cancer cell lines. Also, sulfone 5f was further assessed for its impact on the cell cycle progression and apoptosis in HCT-116 cells.
Aralkanamidophenyl compounds
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, (2008/06/13)
This disclosure describes novel substituted aralkanamidobenzoic acids and analogs thereof. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial wall of mammals.
