title: Piperazine derivatives for therapeutic use: a patent review (2010-present).
abstract: BACKGROUND
  Piperazine, a six membered nitrogen containing heterocycle, is of great significance to the rational design of drugs. This moiety can be found in a plethora of well-known drugs with various therapeutic uses, such as antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardio protectors, anti-inflammatory, and imaging agents. Slight modification to the substitution pattern on the piperazine nucleus facilitates a recognizable difference in the medicinal potential of the resultant molecules.
  
  
  METHODS
  Scifinder was the main source used to search for patents containing piperazine compounds with therapeutic uses. The article describes a variety of molecular designs bearing piperazine entity furnishing CNS agents, anticancer, cardio-protective agents, antiviral, anti-tuberculosis, anti-inflammatory, antidiabetic, and antihistamine profiles, as well as agents relieving pain and useful in imaging applications.
  
  
  CONCLUSIONS
  The great interest gathered to explore piperazine based molecules in relatively few years reflects the broad potential of the entity. Earlier, this scaffold was considered to express CNS activity only. However, a significant increase in research covering studies of several different activities of piperazine ring suggest a successful emergence of the pharmacophore. Certain patents outlined in the present article recommend that piperazines can be a flexible building block to discover drug-like elements and modification of substituents present on the piperazine ring may have a significant impact on the pharmacokinetic and pharmacodynamics factors of the resulting molecules. This article aims to provide insights to piperazine based molecular fragments that would assist drug discoverers to rationally design molecules for various diseases. We anticipate, and highly recommend, further therapeutic investigations on this motif.
authors.affiliation: a Regional Centre of Advanced Technologies and Materials, Faculty of Science, Department of Physical Chemistry , Palacky University , Olomouc , Czech Republic.
authors.forename: Anuj K
authors.initials: AK
authors.lastname: Rathi
authors.affiliation: b Department of Chemistry , J.N.T. University , Hyderabad , India.
authors.forename: Riyaz
authors.initials: R
authors.lastname: Syed
authors.affiliation: c Department of Food Science and Biotechnology, School of Life Science and Biotechnology , Dongguk University , Goyang-si , Republic of Korea.
authors.forename: Han-Seung
authors.initials: HS
authors.lastname: Shin
authors.affiliation: c Department of Food Science and Biotechnology, School of Life Science and Biotechnology , Dongguk University , Goyang-si , Republic of Korea.
authors.forename: Rahul V
authors.initials: RV
authors.lastname: Patel
mesh_terms: D000818:Animals; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods; D006801:Humans; D010330:Patents as Topic; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines
keywords: Anticancer; CNS disorder; anti-inflammatory; anti-tuberculosis; antihistamine; antiviral; cardio-protective; imaging agents; pain; piperazine