A number of fluoroquinolone derivatives were synthesized and evaluated for antimycobacterial activity. Preliminary results are (1) for 1-aryl fluoroquinolones, 1-(4-nitrophenyl) derivatives were inactive while their 1-(2-fluoro-4-nitrophenyl) counterparts were active anti-TB agents (3a vs 4a; 3b vs 4b) indicated the fluoro substituent at C-2 position is important. For the 1-(2-fluoro-4-nitrophe...

The ring opening of some phthalimide derivatives with sodium borohydride in methanol/water (6:1) afforded the corresponding 2-hydroxymethylbenzamides irrespective of the substituents. The most active members of the series evaluated for anti-inflammatory and analgesic activities were 2-hydroxymethyl-N-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethylbenzamide (3d) and 2-hydroxymethyl-N-[4-(2-methoxyphe...

Novel -[4-(2-methoxyphenyl)piperazin-1-yl]ethyl derivatives 1–6 containing 4-, 5and/or 6-arylsubstituted pyrid-2(1H)-one moiety were synthesized. All the new compounds were examined in vitro to assess their 5-HT and 5-HT receptor affinities. Compounds 3 and 4 with a 5or a 6-phenylsubstituted pyridone ring demonstrated high 5-HT receptor affinity (K = 17 and 38 nM, respectively) and were tested ...

Novel omega-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl derivatives 1-6 containing 4-, 5- and/or 6-arylsubstituted pyrid-2(1H)-one moiety were synthesized. All the new compounds were examined in vitro to assess their 5-HT1A and 5-HT2A receptor affinities. Compounds 3 and 4 with a 5- or a 6-phenylsubstituted pyridone ring demonstrated high 5-HT1A receptor affinity (Ki = 17 and 38 nM, respectively) ...

New edaravone derivatives containing a benzylpiperazine moiety are designed and synthesized. The structures characterized by 1 H NMR, 13 C high-resolution mass spectrometry. potential neuroprotective activities of the target compounds evaluated in differentiated rat pheochromocytoma cells (PC12 cells) mice subjected to acute cerebral ischemia. Most showed both vivo vitro, especially 1-(4-(4-flu...

Bu çalışmada, 2,3-di(tiyofen-3-il)piperazin esaslı iletken polimer türevlerinin elektrokimyasal yük depolama özellikleri incelenmiştir. amaçla, ilk önce, ultrases destekli bir yöntem kullanılarak halka sistemine sahip yeni elektroaktif monomerlerin sentezi gerçekleştirilmiştir. 2,3-Di(tiyofen-3-il)piperazin monomerleri olarak paslanmaz çelik substrat yüzeylerinde polimerleştirilmiş ve poli(2,3-...

In the title mol-ecular salt, C(11)H(17)N(2) (+)·Cl(-), the piperazin-1-ium ring adopts a chair conformation with the aromatic ring in a pseudo-equatorial orientation. The dihedral angle between the benzene ring and the mean plane of the piperazin-1-ium ring is 51.22 (6)°. In the crystal, N-H⋯Cl hydrogen bonds link the mol-ecules into chains propagating in [100]. Weak C-H⋯π inter-actions also o...

Based on a known pharmacophore model for 5-HT₆ receptor antagonists, a series of novel extended derivatives of the N-arylsulfonyindole scaffold were designed and identified as a new class of 5-HT₆ receptor modulators. Eight of the compounds exhibited moderate to high binding affinities and displayed antagonist profile in 5-HT₆ receptor functional assays. Compounds 2-(4-(2-methoxyphenyl)piperazi...