- Synthesis of Novel Triazolyl/Oxadiazolyl/Thiadiazolyl-Piperazine as Potential Anticonvulsant Agents
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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
- Archana, Archana
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p. 199 - 203
(2021/01/25)
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- Piperazine-azole-fluoroquinolone hybrids: Conventional and microwave irradiated synthesis, biological activity screening and molecular docking studies
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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
- Mermer, Arif,Faiz, Ozlem,Demirbas, Ahmet,Demirbas, Neslihan,Alagumuthu, Manikandan,Arumugam, Sivakumar
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p. 308 - 318
(2019/01/16)
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- 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
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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
- Mermer, Arif,Bayrak, Hacer,?irin, Yakup,Emirik, Mustafa,Demirba?, Neslihan
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p. 279 - 287
(2019/04/25)
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- Selective, Catalytic, and Dual C(sp3)-H Oxidation of Piperazines and Morpholines under Transition-Metal-Free Conditions
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By using cheap and innocuous reagents, such as NaClO2, NaOCl, and catalytic amounts of TEMPO, a new environmentally friendly protocol for the selective and catalytic TEMPO C(sp3)-H oxidation of piperazines and morpholines to 2,3-diketopiperazines (2,3-DKP) and 3-morpholinones (3-MPs), respectively, has been developed. This novel direct access to 2,3-DKP from piperazines provides significant advantages over the traditional N-monoacylation/intramolecular C-N cyclization procedure. Additionally, by modulating the amounts of TEMPO, 2-alkoxyamino-3-morpholinone can be prepared from morpholine derivatives, which would enable further functionalization at the C2 position of the morpholine skeleton.
- Chamorro-Arenas, Delfino,Osorio-Nieto, Urbano,Quintero, Leticia,Hernández-García, Luís,Sartillo-Piscil, Fernando
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p. 15333 - 15346
(2019/01/03)
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- 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
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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
- Khanam, Rashmin,Kumar, Raj,Hejazi, Iram Iqbal,Shahabuddin, Syed,Meena, Ramovatar,Jayant, Vikrant,Kumar, Prabhat,Bhat, Abdul Roouf,Athar, Fareeda
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p. 113 - 131
(2018/01/27)
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- Design and synthesis of piperazine acetate podophyllotoxin ester derivatives targeting tubulin depolymerization as new anticancer agents
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In this paper, a series of podophyllotoxin piperazine acetate ester derivatives were synthesized and investigated due to their antiproliferation activity on different human cancer cell lines. Among the congeners, C5 manifested prominent cytotoxicity towar
- Sun, Wen-Xue,Ji, Ya-Jing,Wan, Yun,Han, Hong-Wei,Lin, Hong-Yan,Lu, Gui-Hua,Qi, Jin-Liang,Wang, Xiao-Ming,Yang, Yong-Hua
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p. 4066 - 4074
(2017/08/22)
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- PROCASPASE-ACTIVATING COMPOUNDS AND COMPOSITIONS
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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.
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Paragraph 0089-90; 0229-0230
(2013/04/24)
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- Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1)
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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.
- Hsu, Danny C.,Roth, Howard S.,West, Diana C.,Botham, Rachel C.,Novotny, Chris J.,Schmid, Steven C.,Hergenrother, Paul J.
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scheme or table
p. 44 - 50
(2012/03/10)
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- Ruthenium(III) chloride-catalyzed efficient protocol for ethyl diazoacetate insertion into the N-H bond of secondary amines
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Ruthenium(III) chloride (1 mol%) alone can catalyze the insertion of ethyl diazoacetate into N-H bonds of various structurally and electronically diverse secondary cyclic amines under solvent-free conditions to afford the corresponding glycine esters in g
- Varala, Ravi,Enugala, Ramu,Adapa, Srinivas R.
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experimental part
p. 1369 - 1372
(2009/12/04)
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- Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: Binding characterization at D2/D3 receptors and elucidation of a pharmacophore model
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A series of structurally constrained analogues based on hybrid compounds containing octahydrobenzo[g or f]quinoline moieties were designed, synthesized, and characterized for their binding to dopamine D2 and D3 receptors expressed in HEK-293 cells. Among the newly developed constrained molecules, trans-octahydrobenzo[f]quinolin-7-ol (8) exhibited the highest affinity for D2 and D3 receptors, the (-)-isomer being the eutomer. Interestingly, this hybrid constrained version 8 showed significant affinity over the corresponding nonhybrid version 1 (representing a constrained version of the aminotetralin structure only) when assayed under same conditions (Ki of 49.1 and 14.9 nM for 8 vs 380 and 96.0 nM for 1 at D2 and D3, respectively). Similar results were found with other lead hybrid compounds, indicating a contribution of the piperazine moiety in the observed enhanced affinity. On the basis of the data of new lead constrained derivatives and other lead hybrid derivatives developed by us, a unique pharmacophore model was proposed consisting of three pharmacophoric centers, two with aromatic/hydrophobic and one with cationic features.
- Brown, Dennis A.,Kharkar, Prashant S.,Parrington, Ingrid,Reith, Maarten E. A.,Dutta, Aloke K.
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supporting information; experimental part
p. 7806 - 7819
(2009/12/07)
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- Synthesis of substituted piperazinyl semicarbazides and thiosemicarbazide: as possible acetyl cholinesterase (AChE) inhibitors
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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.
- Sengupta,Agarwal,Mushtaq
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p. 961 - 964
(2007/10/04)
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