Preparation of piperazine derivatives as 5-HT7 receptor antagonists

Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives

“…A few related arylsulfamides with a spacer to phenyl-piperazine were testified as active structure for 5-HT 7 antagonist. 20 Considering the importance of benzoxazine-6-sulfonamide, and in continuation of our research program to discover and develop novel biologically active compounds, [21][22][23][24] we have planned to synthesize a new series of compounds having benzoxazine-6-sulfonamide moiety and screened them for their antimicrobial activities. The antibacterial and antifungal activities of all the newly synthesized compounds were evaluated in vitro against one Gram-positive bacterium, three Gram-negative bacteria and one fungus.…”

Synthesis, Spectral Characterization and Antioxidant Activity of Novel Zafirlukast Sulfonyl Derivatives

“…3 Piperazinyl linked ciprofloxacin dimers reported as potent antibacterial agents against resistant strains. 4 Sulfonamide and substituted sulfonamide derivatives are important category of pharmacophores that have a wide spectrum of biological and pharmacological applications such as antimalarial, 5 antimicrobial, 6 antibacterial, 7,8 anticancer, 9 antifungal, 10 antihelmintic, 10 antioxidant, 11 antiHIV, 12 antitumor, 12 antiplasmodial, 13 antineoplastic, 14 antiproliferative 15 activities and additionally known to act as 5-HT 6 , 5-HT 7 receptor antagonists, 16,17 A2B and CXCR3 antagonists, 18,19 11b-HSD, 20 histone deacetylase (HDAC) inhibitors, 21 b-secretase (BACE1) inhibitors 22 and dual PI3K/mTOR inhibitors. 23 In recent years, literature reveals that the research interest and applications of antioxidants have constantly gathered high importance to eradicate the oxidative stress in humans.…”

Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists

“…The reported pharmacophoric hypothesis suggested the minimal structural requirements for 5-HT 2A antagonism consisted of two aryl rings and a basic nitrogen. 13 Based on our previous work, 14 we designed arylsulfonamide derivatives 11-24 and 28 to possess the arylpiperazine moieties as well as a three carbon spacer. …”

“…N-(Cyclopropylmethyl)-3-(4-(4-fluorophenyl)piperazin-1-yl)propan-1-amine (10d). Yellow oil (71%): 1 H (CDCl 3 , 400 MHz) d 6.99-6.95 (m, 2H), 6.89-6.86 (m, 2H), 3.16 (t, J = 4.8 Hz, 4H), 2.79 (s, 4H), 2.74-2.68 (m, 4H), 2.62 (t, J = 4.8 Hz, 2H), 2.09-2.07 (m, 2H), 0.88 (s, 1H), 0.66 (q, J = 7.2 Hz, 2H), 0.32 (q, J = 5.2 Hz, 2H).5.2.4.General procedure for the preparation of N-(R 2 -methyl)-4-methoxy-N-(3-(4-(R 1 -phenyl)piperazin-1-yl)propyl)-Ar-sulfonamide(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24) For the further conversion to sulfonamides, sodium hydride (1 mmol, 2 equiv) was added to a suspension of N-(R 2 -methyl)-3-(4-(R 1 -phenyl)piperazin-1-yl)propan-1-amine 9 and 10 (0.5 mmol, 1 equiv) in DMF (5 mL). After stirring at 60°C for 30 min under nitrogen, Ar-sulfonylchloride (0.75 mmol, 1.5 equiv) in DMF (5 mL) was added.…”