- Design and Synthesis of Novel Piperazine (2-Chloroethyl)-1-nitrosourea Analogues as Anticancer Agents
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A series of piperazine (2-chloroethyl)-1-nitrosourea analogues (6a-h) have been designed, synthesized, characterized and screened for anticancer activity against five human cancer cell lines viz. human colorectal cancer (HCT-116 and HCT-15), human colon cancer (Colo-205), human breast cancer (MCF-7) and leukaemia (Molt-4). Among the screened compounds, compound 6f exhibits potent activity against HCT-116 cell line with an IC50 of 1.0 μM, which regarded as promising drug candidate for the development of anticancer agents.
- Krishnamohan, T.,Kumar, J. V. Shanmukha,Mahesh, Palla,Sowmithri, Sudharshanacharyulu
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p. 591 - 596
(2022/02/22)
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- Synthesis method for co-production of N-hydroxyethyl piperazine and N-ethyl piperazine
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The invention discloses a method for co-production of N-hydroxyethyl piperazine and N-ethyl piperazine. The method comprises the following steps: reacting methyl glycolate serving as a process intermediate for preparing ethylene glycol by a coal method with piperazine to generate an intermediate product carbonyl hydroxyethyl piperazine, then in the presence of a hydrogenation catalyst, carrying out hydrogenation reduction and dehydration under certain pressure and temperature conditions to obtain N-hydroxyethyl piperazine, and simultaneously co-producing part of N-hydroxyethyl piperazine. Themethod is simple and convenient, low in cost, high in total yield, good in selectivity, easy in product separation and environment-friendly.
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Paragraph 0008; 0029-0087
(2021/03/11)
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- Biocatalytic Access to Piperazines from Diamines and Dicarbonyls
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Given the widespread importance of piperazines as building blocks for the production of pharmaceuticals, an efficient and selective synthesis is highly desirable. Here we show the direct synthesis of piperazines from 1,2-dicarbonyl and 1,2-diamine substrates using the R-selective imine reductase from Myxococcus stipitatus as biocatalyst. Various N- and C-substituted piperazines with high activity and excellent enantioselectivity were obtained under mild reaction conditions reaching up to 8.1 g per liter.
- Borlinghaus, Niels,Gergel, Sebastian,Nestl, Bettina M.
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p. 3727 - 3732
(2018/04/14)
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- Synthesis and investigation of novel benzimidazole derivatives as antifungal agents
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The rise and emergence of resistance to antifungal drugs by diverse pathogenic fungal strains have resulted in an increase in demand for new antifungal agents. Various heterocyclic scaffolds with different mechanisms of action against fungi have been investigated in the past. Herein, we report the synthesis and antifungal activities of 18 alkylated mono-, bis-, and trisbenzimidazole derivatives, their toxicities against mammalian cells, as well as their ability to induce reactive oxygen species (ROS) in yeast cells. Many of our bisbenzimidazole compounds exhibited moderate to excellent antifungal activities against all tested fungal strains, with MIC values ranging from 15.6 to 0.975?μg/mL. The fungal activity profiles of our bisbenzimidazoles were found to be dependent on alkyl chain length. Our most potent compounds were found to display equal or superior antifungal activity when compared to the currently used agents amphotericin B, fluconazole, itraconazole, posaconazole, and voriconazole against many of the strains tested.
- Chandrika, Nishad Thamban,Shrestha, Sanjib K.,Ngo, Huy X.,Garneau-Tsodikova, Sylvie
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supporting information
p. 3680 - 3686
(2016/07/20)
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- Characterization of stress degradation products of blonanserin by UPLC-QTOF-tandem mass spectrometry
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Stress studies of drugs are very important in the drug development process. As per regulatory guidelines forced degradation studies and characterization of resulting degradation products is mandatory to establish inherent stability of the drug. Blonanserin is an important drug used for the treatment of schizophrenia. As there are no reports in the literature on the degradation study of the drug, the present work has been undertaken. Blonanserin was subjected to forced degradation studies under the conditions of hydrolysis (acidic, basic and neutral), oxidation, photolysis and thermal stress conditions. A selective separation was achieved on a Waters BEH C18 analytical column (50 mm x 2.1 mm, 1.7 μm). The structural characterization of the degradation products was performed using UPLC/QTOF/MS/MS. The drug was found to degrade in oxidative and photolytic conditions, whereas it was stable under hydrolytic, photolytic and thermal stress conditions. A total of seven hitherto unknown degradation products were characterized and probable mechanisms have been proposed for the formation of the degradation products. Moreover, in silico toxicity of all degradation products was also evaluated.
- Kalariya, Pradipbhai D.,Patel, Prinesh N.,Sharma, Mahesh,Garg, Prabha,Srinivas,Talluri, M. V. N. Kumar
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p. 69273 - 69288
(2015/09/01)
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- METHOD FOR PRODUCING N-MONOALKYL-SUBSTITUTED ALKYLENE AMINE
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PROBLEM TO BE SOLVED: To provide a method for producing an N-monoalkyl-substituted alkylene amine especially useful for uses such as medicine intermediates, agrochemical intermediates, urethane resin-foaming catalysts, surfactants and the like among alkyl-substituted alkylene amine compounds from an alcohol and an alkylene amine as raw materials. SOLUTION: This method for producing the N-monoalkyl-substituted alkylene amine is characterized by reacting the alkylene amine with a ≥2C alkyl alcohol in the presence of a copper-containing oxide catalyst system. The N-monoalkyl-substituted alkylenamine is produced in high conversion and in N-monoalkylation selectivity.
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Page/Page column 8
(2010/02/11)
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- Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics
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Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a-n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity.
- Gao, Feng-Li,Wang, Xin,Zhang, Hong-Mei,Cheng, Tie-Ming,Li, Run-Tao
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p. 1535 - 1537
(2007/10/03)
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- Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction
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There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
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- Catalyst and the amination of alcohols under hydrogenating conditions
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Catalysts whose active material contains, in addition to from 20 to 85% by weight, calculated as ZrO2, of oxygen-containing zirconium compounds, from 1 to 30% by weight, calculated as CuO, of oxygen-containing compounds of copper and from 1 to 40% by weight each, calculated as CoO or NiO, respectively, of oxygen-containing compounds of cobalt and of nickel are used for the amination of alcohols under hydrogenating conditions.
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- ALKYLATION OF ACYCLIC AND CYCLIC DIAMINES AND POLYAMINES
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Alkylation of diamines and polyamines by allyl and methallyl chlorides or by chloropropenes has been used to obtain polyalkylpolyamines that had not been described previously.The alkylation of the polyamines by allyl and methallyl chlorides proceeds more energetically in comparison with the alkylation by ethyl chloride or chloropropenes.The alkylation of either cyclic and acyclic polyamines begins with the primary amino group.With increasing length of the chain and the alkyl radical at the nitrogen of the alkylated polyamines, their capability for reacting with the evolved hydrogen chloride drops off, and this leads to a decrease in yield of the desired products owing to the loss of activity of the original or partly alkylated polyamines.
- Zagudullin, R. N.,Baimetov, Z. M.
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p. 889 - 894
(2007/10/02)
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- CATALYTIC SYNTHESIS OF DIAZINES FROM 1,3-DIAMINOPROPANE AND 3-AMINO-1-PROPANOL
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The transformation of 1,3-diaminopropane and 3-amino-1-propanol under pulse conditions over tungsten trioxide in an inert atmosphere at 300-500 deg C were investigated.The transformation of 1,3-diaminopropane leads to the formation of saturated pyrimidine
- Oshis, Ya. F.,Anderson, A. A.,Shimanskaya, M. V.
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p. 740 - 745
(2007/10/02)
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- Use of cyclic thiazines as microbiocides
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Cyclic thiazines of the formula STR1 where the R's are hydrogen or a substituted group such as a hydrocarbon group, i.e., alkyl, etc. and N is a cyclic moiety, Z is S, STR2 and X is an anion, are prepared by reacting a cyclic secondary amine salt with a divinyl sulfur compound. These are illustrated by the reaction of piperidine hydrochloride with divinyl sulfone to yield STR3 These products have a wide variety of uses including their use as microbiocides, etc.
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- Pharmaceutical compositions and methods of inhibiting gastric acid secretion
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Pharmaceutical compositions and methods of inhibiting gastric acid secretion by administering N-alkenyl and N-alkynyl thioamides.
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- N-aminomethyl-2-amino(and 2-amino-methyl)-2-(2-quinolyl)-thioacetamides
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The compounds are N-aminomethyl-2-amino(and 2-aminomethyl)-2-heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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