- New oxime reactivators connected with CH2O(CH2)nOCH2 linker and their reactivation potency for organophosphorus agents-inhibited acetylcholinesterase
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New bis-pyridinium oxime reactivators 6 with CH2O(CH2)2OCH2 and CH2O(CH2)4OCH2 linkers between the two pyridinium rings were designed and synthesized. In the in vitro test of their potency to reactivate AChE inhibited by organophosphorus agents at 5 × 10-3 M concentration, the reactivation ability of 1,2-dimethoxy-ethylene-bis-N,N′-4-pyridiumaldoxime dichloride (6a) was 63% for housefly (HF) AChE inhibited by diisopropyl fluorophosphates (DFP), 51% for bovine red blood cell (RBC) AChE inhibited by DFP, 67% for HF-AChE inhibited by paraoxon, and 81% for RBC-AChE inhibited by paraoxon. Except in the case of DFP-inhibited HF AChE test of 2-PAM, the activities of 6a are much higher than the activities of 2-PAM and HI-6 which are AChE reactivators currently in use.
- Yang, Garp Yeol,Oh, Kyung-Ae,Park, No-Joong,Jung, Young-Sik
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- Antimicrobial activity and SAR study of new gemini imidazolium-based chlorides
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A series of 70 new 3,3′(α,ω-dioxaalkyl)bis(1- alkylimidazolium) chlorides were synthesized. They were characterized with respect to surface active properties and antimicrobial activity against the following pathogens: Staphylococcus aureus, Enterococcus faecalis, Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa, Candida krusei, and Candida albicans. In this article, besides description of the synthesis, we characterize a set of features of these compounds, concerning their structure (described by the length of the dioxaalkan spacer and the length of the alkyl substituent in the aromatic ring) and surface active properties (critical micelle concentration, value of surface tension at critical micelle concentration, value of surface excess, molecular area of a single particle, and free energy of adsorption of molecule). Then, we present a SAR study for Staphylococcus aureus, as one of the most widespread pathogenic strains, conducted with the help of the Dominance-based Rough Set Approach (DRSA), that involves identification of relevant features and relevant combinations of features being in strong relationship with a high antimicrobial activity of the compounds. The SAR study shows, moreover, that the antimicrobial activity is dependent on the type of substituents and their position at the chloride moiety, as well as on the surface active properties of the compounds.
- Pa?kowski, ?ukasz,B?aszczyński, Jerzy,Skrzypczak, Andrzej,B?aszczak, Jan,Kozakowska, Karolina,Wróblewska, Joanna,Kozuszko, Sylwia,Gospodarek, Eugenia,Krysiński, Jerzy,S?owiński, Roman
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- TRINITROETHYL ETHERS OF SUBSTITUTED ALCOHOLS
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The influence of the trinitromethane salt cations and the substituents in the alkyl moiety of chloromethyl ethers of alcohols on the yields of trinitroethyl ethers of the substituted alcohols formed from them was established.On this basis a representative series of previously unavailable trinitroethanol ethers was synthesized.
- Luk'yanov, O.A.,Pokhvisneva, G.V.
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- Synthesis of 9,9'-[1,2-Ethanediylbis(oxymethylene)]bis-2-amino- 1,9-dihydro-6H-purin-6-one, an impurity of acyclovir
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The synthesis of 9,9'-[1,2-ethanediylbis(oxymethylene)]bis-2-amino-1,9- dihydro- 6H-purin-6-one, a minor impurity of acyclovir, is described. Starting with commercial N-(9-acetyl-6-oxo-1H-purin-2-yl)acetamide, the process uses an acid catalysed phase transfer catalysis (PTC) process to produce the selective alkylation at the 9 position of the guanine ring.
- Suarez, Rosa M.,Matia, Maria Paz,Novella, Jose Luis,Molina, Andres,Cosme, Antonio,Vaquero, Juan Jose,Alvarez-Builla, Julio
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p. 8735 - 8741
(2012/11/07)
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- Design, synthesis and biological characterization of novel inhibitors of CD38
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Human CD38 is a novel multi-functional protein that acts not only as an antigen for B-lymphocyte activation, but also as an enzyme catalyzing the synthesis of a Ca2+ messenger molecule, cyclic ADP-ribose, from NAD+. It is well established that this novel Ca2+ signaling enzyme is responsible for regulating a wide range of physiological functions. Based on the crystal structure of the CD38/NAD+ complex, we synthesized a series of simplified N-substituted nicotinamide derivatives (Compound1-14). A number of these compounds exhibited moderate inhibition of the NAD+ utilizing activity of CD38, with Compound4 showing the highest potency. The crystal structure of CD38/Compound4 complex and computer simulation of Compound7 docking to CD38 show a significant role of the nicotinamide moiety and the distal aromatic group of the compounds for substrate recognition by the active site of CD38. Biologically, we showed that both Compounds4 and 7 effectively relaxed the agonist-induced contraction of muscle preparations from rats and guinea pigs. This study is a rational design of inhibitors for CD38 that exhibit important physiological effects, and can serve as a model for future drug development.
- Dong, Min,Si, Yuan-Qi,Sun, Shuang-Yong,Pu, Xiao-Ping,Yang, Zhen-Jun,Zhang, Liang-Ren,Zhang, Li-He,Leung, Fung Ping,Lam, Connie Mo Ching.,Kwong, Anna Ka Yee,Yue, Jianbo,Zhou, Yeyun,Kriksunov, Irina A.,Hao, Quan,Cheung Lee, Hon
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p. 3246 - 3257
(2011/06/10)
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- POLYMER COMPOUND, PHOTORESIST COMPOSITION CONTAINING SUCH POLYMER COMPOUND, AND METHOD FOR FORMING RESIST PATTERN
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A polymer compound that, within a chemically amplified positive resist system, exhibits a significant change in alkali solubility from a state prior to exposure to that following exposure, as well as a photoresist composition that includes such a polymer compound and a method for forming a resist pattern, which are capable of forming fine patterns with a high level of resolution. The polymer compound includes, as an alkali-soluble group (i), a substituent group in which a group selected from amongst alcoholic hydroxyl groups, carboxyl groups, and phenolic hydroxyl groups is protected with an acid dissociable, dissolution inhibiting group (ii) represented by a general formula (1) shown below: (wherein, A represents an organic group of 1 to 20 carbon atoms with a valency of at least n+1, and n represents an integer from 1 to 4).
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