40782-58-9Relevant academic research and scientific papers
Supramolecular synthons and pattern recognition in adenine amides - Synthesis, structures and thermal properties
Adamski, Ariel,Bogucki, Andrzej,?wietlik, Roman,Wróbel, Rafa? J.,Klapiszewski, ?ukasz,Jesionowski, Teofil,Tylkowski, Bartosz,Kubicki, Maciej,Patroniak, Violetta
, p. 571 - 583 (2015)
An effective method for the synthesis of novel adenine amides was developed and successfully implemented, leading to 4-propyloxy-N-(9H-purin-6-yl)benzamide (1) and 4-dodecyloxy-N-(9H-purin-6-yl)benzamide (2). The compounds were fully characterised by mean
Synthesis of new metallomesogens with enaminoketone chelating ligands
Kovganko,Kovganko
, p. 907 - 911 (2006)
New liquid crystalline copper(II) enaminoketonates containing bridging ester groups were synthesized by hydrogenation of the heteroring in 3-(4-hydroxyphenyl)-5-pentylisoxazole to 1-amino-1-(4-hydroxyphenyl)oct-1-en-3- one, treatment of the latter with co
Lappaconitine derivative with analgesic activity, and preparation method and application thereof
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Paragraph 0286-0291, (2021/07/14)
The invention provides a lappaconitine derivative with analgesic activity, and a preparation method and application thereof. The structure of the lappaconitine derivative is as shown in formula I in the specification. The lappaconitine derivative provided by the invention is high in analgesic activity, good in water solubility and low in biotoxicity, can be used for preparing low-toxicity analgesic drugs, and is wide in application prospect.
Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis
Darwish, Salma,Erdmann, Frank,Ghazy, Ehab,Heimburg, Tino,Jung, Manfred,Lancelot, Julien,Pierce, Raymond,Robaa, Dina,Romier, Christophe,Schmidt, Matthias,Schmidtkunz, Karin,Shaik, Tajith B.,Simoben, Conrad V.,Sippl, Wolfgang,Truhn, Anne,Zeyen, Patrik
, (2021/08/17)
Schistosomiasis is a major neglected parasitic disease that affects more than 265 million people worldwide and for which the control strategy consists of mass treatment with the only available drug, praziquantel. In this study, we chemically optimized our previously reported benzhydroxamate-based inhibitors of Schistosoma mansoni histone deacetylase 8 (smHDAC8). Crystallographic analysis provided insights into the inhibition mode of smHDAC8 activity by the highly potent inhibitor 5o. Structure-based optimization of the novel inhibitors was carried out using the available crystal structures as well as docking studies on smHDAC8. The compounds were evaluated in screens for inhibitory activity against schistosome and human HDACs (hHDAC). The in vitro and docking results were used for detailed structure activity relationships. The synthesized compounds were further investigated for their lethality against the schistosome larval stage using a fluorescence-based assay. The most promising inhibitor 5o showed significant dose-dependent killing of the schistosome larvae and markedly impaired egg laying of adult worm pairs maintained in culture.
Synthesis and characterization of novel rod-like ester-based liquid crystalline homologous series: Effect of tert-butyl tail on mesomorphism
Thakur, Shavi,Patel, Hemant N.
, p. 76 - 89 (2021/04/14)
A new rod-like homologous series consisting twelve compounds with central ester linkage and terminal tert-butyl group, tert-butyl [4-(4’-n-alkoxybenzoyloxy)benzoates] has been synthesized and characterized through standard spectroscopic techniques like UV, FT-IR, 1HNMR, DSC, POM, and XRD. Methoxy and ethoxy derivatives are nonmesogenic. Nematic mesophase commences as enantiotropy from propyloxy derivative and persists up to the octadecyloxy derivatives. Smectic A mesophase commences as monotropy from propyloxy to the octadecyloxy derivatives. The mesomorphic properties of present series are compared with other structurally related series to evaluate the effect of terminal tert-butyl group on mesomorphism. Two derivatives are subjected to in?vitro antimicrobial activity.
Synthesis and Mesomorphic Properties of Novel Bent-shaped Naphthyl Diketones
Buljan, An?ela,Kne?evi?, Anamarija,Dokli, Irena,Lesac, Andreja
, p. 173 - 179 (2019/12/12)
The synthesis and liquid-crystalline properties are reported for novel naphthyl-based diketones incorporating variant terminal chains and lateral fluoro- substitution. Newly prepared materials exhibit a broad temperature range of the nematic phase. The study demonstrates how subtle structural modifications can be exploited to alter the efficiency of molecular packing and consequently the thermal behaviour.
Dependence of mesomorphism on terminal polar group in novel azoester series
Kher, Seema N.,Prajapati,Makwana,Chandra, Raviprakash S.
, p. 44 - 53 (2019/10/14)
Novel homologous series 4-(4′-n-alkoxy benzoyloxy) napthyl azo 4″–bromo benzenes, consisted of 11 members of a series. All the 11 members (ethoxy to hexadecyloxy) except hexadecyloxy are only enantiotropically nematogenic without exhibition of any smectogenic character. Transition temperatures and the textures are determined by an optical polarizing microscopy equipped with a heating stage. Textures of a nematic phase are threaded or schlieren. Analytical and spectral data supported the molecular structure of homologs. Transition curves viz., solid-nematic and nematic-isotropic showing phase behavior of the mesophase in a phase diagram behave in normal manner. Alternation of transition temperatures is exhibited by N–I transition curve. Thus, novel series is entirely nematogenic and high ordered melting type. Thus, synthesis of a novel azoester homologous series is carried out with a view to understand and establish the effect of molecular structure on Liquid crystal (LC) behaviors of a substance.
Identification of Anti-Mycobacterial Biofilm Agents Based on the 2-Aminoimidazole Scaffold
Nguyen, T. Vu,Minrovic, Bradley M.,Melander, Roberta J.,Melander, Christian
, p. 927 - 937 (2019/03/26)
Tuberculosis (TB) remains a significant global health problem for which new therapeutic options are sorely needed. The ability of the causative agent, Mycobacterium tuberculosis, to reside within host macrophages and form biofilm-like communities contributes to the persistent and drug-tolerant nature of the disease. Compounds that can prevent or reverse the biofilm-like phenotype have the potential to serve alongside TB antibiotics to overcome this tolerance, and decrease treatment duration. Using Mycobacterium smegmatis as a surrogate organism, we report the identification of two new 2-aminoimidazole compounds that inhibit and disperse mycobacterial biofilms, work synergistically with isoniazid and rifampicin to eradicate preformed M. smegmatis biofilms in vitro, are nontoxic toward Galleria mellonella, and exhibit stability in mouse plasma.
Study of Y-shaped liquid crystalline materials with polar nitro substituent
Dixit, Sandhya
, p. 77 - 84 (2018/06/27)
A new homologous series of Y-shaped liquid crystals namely 4-Nitro-[2′4′bis (4″-n-alkoxybenzoyloxy)] phenyl bisazobenzenes have been synthesized and its thermotropic properties studied on the hot stage of a polarizing microscope. The compounds consist four phenyl rings joined through ester and bisazo linkages with alkoxy and nitro as terminal substituents. The structures of synthesized compounds were confirmed by spectroscopic techniques such as FTIR, 1HNMR as well as elemental analysis. The compounds were found to exhibit enantiotropic nematic and smectic mesophases. The role of molecular shape, size and polarity of functional groups in the mesophases formation is discussed.
Mesomorphism dependence on terminal polar group in the nonlinear novel azoester series
Kher, Seema N.,Prajapati,Chandra, Raviprakash S.,Makwana
, p. 1 - 9 (2019/02/24)
Synthesis of a novel azoester homologous series is carried out with a view to understand and establish the effect of molecular structure on liquid crystal (LC) behaviors of a substance. Novel series consists of ten LC substances. All the homologs are enantiotropically nematogenic without exhibition of smectic property. Transition and melting temperatures, textures of LC are determined by an optical polarizing microscopy equipped with a heating stage. Textures of nematic phase are threaded or schlieren. Transition curves of a phase diagram behaved in normal manner. Nematic–isotropic transition curve exhibited odd–even effect. Analytical and spectral data supported and confirmed the structures of homologues.
