- Sensitive Analysis of Nitroguanidine in Aqueous and Soil Matrices by LC-MS
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Nitroguanidine, a widely used nitramine explosive, is an environmental contaminant that is refractory, persistent, highly mobile in soils and aquifers, and yet under-researched. Nitroguanidine determination in water and soil poses an analytical challenge due its high hydrophilicity, low volatility, charge neutrality over a wide pH range, and low proton affinity which results in low electrospray interface (ESI)-MS sensitivity. A sensitive method for the determination of nitroguanidine in aqueous and soil matrices was developed. The method is based on reduction by zinc in acidic solution, hydrophobization by derivatization, preconcentration on C18 cartridge, and LC-MS quantification. The demonstrated limit of detection (LOD) reaches 5 ng/L and 22 ng/g in water and soil, respectively. Analysis of a contaminated site demonstrates that it is possible to map a contamination plume that extends over 1 km from the source of the contamination.
- Voloshenko Rossin, Anna,Sladkevich, Sergey,Gasser, Guy,Melman, Artem,Lev, Ovadia
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- Synthesis, Antileishmanial Activity and In Silico Studies of Aminoguanidine Hydrazones (AGH) and Thiosemicarbazones (TSC) Against Leishmania chagasi Amastigotes
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Background: Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Among the four main clinical forms of the disease, visceral leishmaniasis is the most se-vere, fatal in 95% of cases. The undesired side-effects from first-li
- Alexandre-Moreira, Magna S.,Aquino, Pedro G. V.,Bourguignon, Jean-Jacques,Bri-Card, Jacques,Freitas, Johnnatan D.,Meneghetti, Mario R.,Nascimento, Igor J. S.,Queiroz, Aline C.,Rodrigues, Klinger A. F.,Rodrigues, Raiza R. L.,Santos, Mariana S.,Schmitt, Martine,de Aquino, Thiago M.,Araújo, Morgana V.,Fran?a, Paulo H. B.,Rodrigues, érica E. E. S.,Santos-Júnior, Paulo F. S.,da Silva-Júnior, Edeildo F.,de Araújo-Júnior, Jo?o X.
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p. 151 - 169
(2022/02/05)
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- Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors
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Herein we report a microscale parallel synthetic approach allowing for rapid access to libraries of N-acylated aminotriazoles and screening of their inhibitory activity against factor XIIa (FXIIa) and thrombin, which are targets for antithrombotic drugs. This approach, in combination with post-screening structure optimization, yielded a potent 7 nM inhibitor of FXIIa and a 25 nM thrombin inhibitor; both compounds showed no inhibition of the other tested serine proteases. Selected N-acylated aminotriazoles exhibited anticoagulant properties in vitro influencing the intrinsic blood coagulation pathway, but not extrinsic coagulation. Mechanistic studies of FXIIa inhibition suggested that synthesized N-acylated aminotriazoles are covalent inhibitors of FXIIa. These synthesized compounds may serve as a promising starting point for the development of novel antithrombotic drugs.
- Platte, Simon,Korff, Marvin,Imberg, Lukas,Balicioglu, Ilker,Erbacher, Catharina,Will, Jonas M.,Daniliuc, Constantin G.,Karst, Uwe,Kalinin, Dmitrii V.
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supporting information
p. 3672 - 3690
(2021/08/07)
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- Synthesis of 5 - amino tetrazole method
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Synthesis of 5 - amino tetrazole method, in order to hydrazine hydrate, lime nitrogen, sodium nitrite, inorganic acid and inorganic base as the obtained 5 - amino tetrazole. The method through the metathesis reaction, addition reaction and diazo isomerization reaction of the cyano lead lime nitrogen into the aminoguanidine, then generating aminoguandine isomerization reaction to synthesize 5 - amino tetrazole. The invention compared with the traditional method, has the following advantages: (1) price cheap raw materials as the starting raw material, synthetic product is obtained; (2) simplified 5 - amino tetrazole operation process, reduce the reaction solvent types and process the complexity of the operation, reduces the cost of material and production cost, reduces the 5 - amino tetrazole synthesis cost of, improve the market competitiveness of the product. It has high efficiency, high yield, low cost, easy operation and the like.
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Paragraph 0028; 0029; 0030
(2019/06/13)
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- Glycation Cross-link Breakers to Increase Resistance to Enzymatic Degradation
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The present invention relates to a method to treat a grafts, implant, scaffold, and constructs, including allografts, xenografts, autografts, and prosthetics comprising collagen, with an inhibitor of collagen cross-links and/or advanced glycation endproducts (AGE), in order to alleviate the mechanical weakness induced by the cross-links The invention also provides for kits for use in the operating theater during autograft, allograft or xenograft procedures, or for preparing allograft, xenografts or prosthetics that have not been already treated prior to packaging. The kit comprises a first agent or agents that inhibit collagen cross-links and/or advanced glycation endproducts, instructions for use, optionally a wash or rinse agent, and a device for containing the graft and first agent.
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- PROCESS FOR STRAIGHTENING KERATIN FIBRES WITH A HEATING MEANS AND DENATURING AGENTS
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The invention relates to a process for straightening keratin fibres, comprising: (i) a step in which a straightening composition containing at least two denaturing agents is applied to the keratin fibres, (ii) a step in which the temperature of the keratin fibres is raised, using a heating means, to a temperature of between 110 and 250° C.
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- Dinitropyrazolopyrazole-amine salts useful in gun propellants
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Dinitropyrazolopyrazole-amine salts are used as burn modifier ingredients in gun propellant compositions.
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Page column 3; 4
(2008/06/13)
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- Low molecular weight bicyclic thrombin inhibitors
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This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
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- Antiarrhythmic active amidinohydrazones of substituted benzophenones. Part 5: Investigations on the stability of (Z)-2-amino-5-chlorobenzophenonamidinohydrazone acetate in solution
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The aqueous solution of the title compound can be used for injection for one year if it is stored at room temperature and under light protection. Under these conditions 8% of the E-isomer are produced. The reaction is reversible at day light. Red coloured products of decomposition are formed by long lasting influence of light. At higher temperatures or at sterilisation several products of decomposition are formed which structure is elucidated. For these decomposition a scheme is proposed.
- Schleuder,Richter,Keckeis,Jira
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- 3-aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives, their salts, a process for their preparation, agents containing them and their use
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3-Aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives of the formula I STR1 and their physiologically tolerated acid addition and ammonium salts are described, as is a process for their preparation. The new compounds are chemotherapeutic agents and are active against protozoa, especially malaria plasmodia.
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- Process for producing N-phosphonomethylglycine acid
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The invention provides a process for producing N-phosphonomethylglycine acid (NPMG) comprising (a) oxidizing an N-(phosphonomethyl) iminodiacetic acid (NPMIDA) derivative of the general formula I STR1 wherein n is 1 or 2 and R5, R5', R6 and R6' are independently H, NH2, STR2 or an aryl, cycloalkyl or straight or branched chain alkyl or alkenyl group optionally substituted by hydroxy or halogen, or an alkylaryl group, provided that at least one of R5, R5 ', R6 or R6 ' is hydrogen, to produce a corresponding iminourea salt of NPMG and then (b) reacting the salt with an acid stronger than NPMG whereby NPMG is produced and there remains in solution the iminourea salt of the stronger acid.
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- Guanylhydrazones and medicaments containing them
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New guanylhydrazones of phenoxyacetic acid. These guanylhydrazones, also their physiologically acceptable salts, are characterized by the following general formula I in which R1, R2, R3, R4, R5, R and R' have the meanings which are hereinafter described. STR1 The new guanylhydrazones are useful as medicaments, in particular antimitotic, IMAO and platelet antiagregant activity.
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- Benzoquinolizines having blood pressure lowering activity, and in some instances, anti-secretory activity
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The invention concerns benzoquinolizines of the general formula (I) STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein R1 and R2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen and R represents --CXNHR3 (where X is O, S or =NH and R3 is hydrogen or lower alkyl) or --(CH2)n R4 (where n is 0 or 1 and R4 is aryl). These compounds lower blood pressure. Some are also anti-ulcer agents. The compounds in which R1, R2 and R are as defined above, with the proviso that when R is phenyl, R1 and R2 are not both lower alkoxy, are novel.
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