1689-05-0Relevant articles and documents
Synthesis of novel Azol-β-lactam derivatives starting from phenyl piperazine and investigation of their antiurease activity and antioxidant capacity comparing with their molecular docking studies
Mermer, Arif,Bayrak, Hacer,?irin, Yakup,Emirik, Mustafa,Demirba?, Neslihan
, p. 279 - 287 (2019)
This study reports the synthesis, biological investigation and molecular docking of novel β-lactam derivatives bearing 1,3,4-thiadiazole and 1,3,4-oxadiazole ring system. The synthesized compounds were evaluated for in vitro antiurease activity and antiox
Synthesis of Novel Triazolyl/Oxadiazolyl/Thiadiazolyl-Piperazine as Potential Anticonvulsant Agents
Archana, Archana
, p. 199 - 203 (2021/01/25)
Reaction of piperazine with chloroacetylchloride in dry acetone yield compound 1, which on reaction with hydrazine hydrate yielded compound 2, which was further reacted with various substituted phenylisothiocyanates in absolute alcohol to afford compounds
Piperazine-azole-fluoroquinolone hybrids: Conventional and microwave irradiated synthesis, biological activity screening and molecular docking studies
Mermer, Arif,Faiz, Ozlem,Demirbas, Ahmet,Demirbas, Neslihan,Alagumuthu, Manikandan,Arumugam, Sivakumar
, p. 308 - 318 (2019/01/16)
A series of new 1,2,4-triazole and 1,3,4-oxadiazole derivatives was obtained via several steps sequential reactions of phenyl piperazine. Then, these compounds were converted to the corresponding fluoroquinolone hybrids via one pot three component Mannich
Piperazine clubbed with 2-azetidinone derivatives suppresses proliferation, migration and induces apoptosis in human cervical cancer HeLa cells through oxidative stress mediated intrinsic mitochondrial pathway
Khanam, Rashmin,Kumar, Raj,Hejazi, Iram Iqbal,Shahabuddin, Syed,Meena, Ramovatar,Jayant, Vikrant,Kumar, Prabhat,Bhat, Abdul Roouf,Athar, Fareeda
, p. 113 - 131 (2018/01/27)
Abstract: Piperazine scaffolds or 2-azetidinone pharmacophores have been reported to show anti-cancer activities and apoptosis induction in different types of cancer cells. However, the mechanistic studies involve in induction of apoptosis addressing thes
PROCASPASE-ACTIVATING COMPOUNDS AND COMPOSITIONS
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Paragraph 0091-0092; 0232-0233, (2013/04/24)
The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1)
Hsu, Danny C.,Roth, Howard S.,West, Diana C.,Botham, Rachel C.,Novotny, Chris J.,Schmid, Steven C.,Hergenrother, Paul J.
scheme or table, p. 44 - 50 (2012/03/10)
Procaspase-Activating Compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazone that enhances the enzymatic activity of procaspase-3 in vitro and induces apoptosis in cancer cells. An analogue of PAC-1, called S-PAC-1, was evaluated in a veterinary clinical trial in pet dogs with lymphoma and found to have considerable potential as an anticancer agent. With the goal of identifying more potent compounds in this promising class of experimental therapeutics, a combinatorial library based on PAC-1 was created, and the compounds were evaluated for their ability to induce death of cancer cells in culture. For library construction, 31 hydrazides were condensed in parallel with 27 aldehydes to create 837 PAC-1 analogues, with an average purity of 91%. The compounds were evaluated for their ability to induce apoptosis in cancer cells, and through this work, six compounds were discovered to be substantially more potent than PAC-1 and S-PAC-1. These six hits were further evaluated for their ability to relieve zinc-mediated inhibition of procaspase-3 in vitro. In general, the newly identified hit compounds are two- to four-fold more potent than PAC-1 and S-PAC-1 in cell culture, and thus have promise as experimental therapeutics for treatment of the many cancers that have elevated expression levels of procaspase-3.
Synthesis of substituted piperazinyl semicarbazides and thiosemicarbazide: as possible acetyl cholinesterase (AChE) inhibitors
Sengupta,Agarwal,Mushtaq
, p. 961 - 964 (2007/10/04)
Some new N'-(N-aryl-N'-acetyl) piperazine-N4-aryl/alkyl semicarbazide and thiosemicarbazides have been synthesised as possible acetyl cholinesterase (AChE) inhibitors, by the condensation of N-aryl N'-piperazine acetic acid hydrazide with aryl or alkyl isocyanate and aryl isothiocyanates.