The 7-chloro-4-(piperazin-1-yl)quinoline structure is an important scaffold in medicinal chemistry. It exhibited either alone or as hybrid with other active pharmacophores diverse pharmacological profiles such as: antimalarial, antiparasitic, anti-HIV, antidiabetic, anticancer, sirtuin Inhibitors, dopamine-3 ligands, acetylcholinesterase inhibitors, and serotonin antagonists. In the presented review, a comprehensive discussion of compounds having this structural core is surveyed and illustrated.

• Klíčová slova
• 7-chloro-4-(piperazin-1-yl)quinoline, anti-HIV, anticancer, antidiabetic, antimalarial,
• MeSH
• chinoliny chemie   farmakologie   MeSH
• lidé MeSH
• vztahy mezi strukturou a aktivitou MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• chinoliny MeSH

This study evaluated the effect of age and renal impairment on pharmacokinetics of trimetazidine (TMZ) in healthy elderly and renally impaired subjects and assess safety and tolerability. In this open-label, multi-dose study, 73 subjects were divided into six treatment groups: (1) 55-65 years; (2) 66-75 years; (3) >75 years (dosing for groups 1-3 [healthy]: B.D. for 4 days), (4) mild renally impaired (dosed B.D. for 8 days); (5) moderate renally impaired (dosed O.D. for 8 days); and (6) severe renally impaired-no dialysis (dosed once every 48 h for 8 days). Blood and urine samples were collected and analyzed. The geometric least squares mean ratios for; Group 2 and 1 of AUC(0-τ)ss was 112.2 (90% CI; 92.0-136.8) and Cmax,ss was 109.9 (89.6-134.8), Group 3 and 1 of AUC(0-τ),ss was 140.5 (115.9-170.3) and Cmax,ss was 137.8 (112.9-168.2), Group 4 and 1 of AUC(0-τ),ss was 114.2 (90.3-144.4) and Cmax,ss was 120.8 (92.5-157.8), Group 5 and 1 of; AUC(0-τ),ss was 213.0 (153.1-296.3) and Cmax,ss was 123.3 (92.2-164.7) and Group 6 and 1 of AUC(0-τ),ss was 247.4 (197.8-309.6) and Cmax,ss was 95.6 (73.0-125.1). Significant increase in systemic exposure of TMZ was observed in subjects; over 75 year's age and renally impaired compared to healthy subjects. TMZ was safe and well-tolerated.

• Klíčová slova
• age, pharmacokinetics, renal-impairment, safety, tolerability, trimetazidine,
• MeSH
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• renální insuficience krev   metabolismus   MeSH
• senioři nad 80 let MeSH
• senioři MeSH
• trimetazidin škodlivé účinky   krev   farmakokinetika   MeSH
• vazodilatancia škodlivé účinky   krev   farmakokinetika   MeSH
• věkové faktory MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři nad 80 let MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• klinické zkoušky kontrolované MeSH
• multicentrická studie MeSH
• práce podpořená grantem MeSH
• Názvy látek
• trimetazidin MeSH
• vazodilatancia MeSH