- New pyrimidine-benzoxazole/benzimidazole hybrids: Synthesis, antioxidant, cytotoxic activity, in vitro cyclooxygenase and phospholipase A2-V inhibition
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To enhance the cytotoxicity of benzimidazole and/or benzoxazole core, the benzimidazole/benzoxazole azo-pyrimidine were synthesized through diazo-coupling of 3-aminophenybenzimidazole (6a) or 3-aminophenylbenzoxazole (6b) with diethyl malonate. The new az
- Abdelgawad, Mohamed A.,Bakr, Rania B.,Ahmad, Waqas,Al-Sanea, Mohammad M.,Elshemy, Heba A.H.
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- Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors
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In the present study, we attempted to develop novel class of Mycobacterium tuberculosis (Mtb) inhibitors by exploring the pharmaceutically underexploited enzyme targets which are majorly involved in cell wall biosynthesis of mycobacteria. For this purpose
- Malapati, Prasanthi,Krishna, Vagolu Siva,Nallangi, Radhika,Srilakshmi, Rudraraju Reshma,Sriram, Dharmarajan
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- Discovery and computational studies of 2-phenyl-benzoxazole acetamide derivatives as promising P2Y14R antagonists with anti-gout potential
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The P2Y14 nucleotide receptor, a subtype of P2Y receptors, is implicated in many human inflammatory diseases. Based on the identification of favorable residues of two screening hits in the almost symmetrical P2Y14 binding domain, we
- Zhou, Mengze,Wang, Weiwei,Wang, Zhongkui,Wang, Yilin,Zhu, Yifan,Lin, Zhiqian,Tian, Sheng,Huang, Yuan,Hu, Qinghua,Li, Huanqiu
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- A Diverse Range of Hemozoin Inhibiting Scaffolds Act on Plasmodium falciparum as Heme Complexes
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A diverse series of hemozoin-inhibiting quinolines, benzamides, triarylimidazoles, quinazolines, benzimidazoles, benzoxazoles, and benzothiazoles have been found to lead to exchangeable heme levels in cultured Plasmodium falciparum (NF54) that ranged over an order of magnitude at the IC50. Surprisingly, less active compounds often exhibited higher levels of exchangeable heme than more active ones. Quantities of intracellular inhibitor measured using the inoculum effect exhibited a linear correlation with exchangeable heme, suggesting formation of heme-inhibitor complexes in the parasite. In an effort to confirm this, the presence of a Br atom in one of the benzimidazole derivatives was exploited to image its distribution in the parasite using electron spectroscopic imaging of Br, an element not naturally abundant in cells. This showed that the compound colocalized with iron, consistent with its presence as a heme complex. Direct evidence for this complex was then obtained using confocal Raman microscopy. Exchangeable heme and inhibitor were found to increase with decreased rate of killing, suggesting that slow-acting compounds have more time to build up exchangeable heme complexes. Lastly, some but not all compounds evidently cause pro-oxidant effects because their activity could be attenuated with N-acetylcysteine and potentiated with t-butyl hydroperoxide. Collectively, these findings suggest that hemozoin inhibitors act as complexes with free heme, each with its own unique activity.
- Openshaw, Roxanne,Maepa, Keletso,Benjamin, Stefan J.,Wainwright, Lauren,Combrinck, Jill M.,Hunter, Roger,Egan, Timothy J.
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p. 362 - 376
(2021/02/01)
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- Novel Phenolic Compounds as Potential Dual EGFR and COX-2 Inhibitors: Design, Semisynthesis, in vitro Biological Evaluation and in silico Insights
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Introduction: Epidermal growth factor receptor (EGFR) inhibition is an imperative therapeutic approach targeting various types of cancer including colorectal, lung, breast, and pancreatic cancer types. Moreover, cyclooxygenase-2 (COX-2) is frequently over
- Abdelgawad, Mohamed A.,Ahmad, Waqas,Al-Muaikel, Nayef S.,Al-Sanea, Mohammad M.,Alanazi, Abdullah S.,Alharbi, Metab,Almalki, Atiah H.,Alzarea, Sami I.,Bakr, Rania B.,Bukhari, Syed N. A.,Ghoneim, Mohammed M.,Hegazy, Mostafa M.,Mostafa, Ehab M.,Mostafa-Hedeab, Gomaa,Musa, Arafa,Parambi, Della G. T.
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p. 2325 - 2337
(2022/01/13)
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- Benzoxazole derivative as well as preparation method and application thereof (by machine translation)
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The invention provides a benzoxazole derivative as well as a preparation method and application, of the benzoxazole derivative as P. 2 Y14 The inhibitor has good inhibitory activity and anti-inflammatory activity, and further, by res
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Paragraph 0029-0033
(2020/03/29)
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- 2-Aryl benzazole derived new class of anti-tubercular compounds: Endowed to eradicate mycobacterium tuberculosis in replicating and non-replicating forms
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The high mortality rate and the increasing prevalence of Mtb resistance are the major concerns for the Tuberculosis (TB) treatment in this century. To counteract the prevalence of Mtb resistance, we have synthesized 2-aryl benzazole based dual targeted molecules. Compound 9m and 9n were found to be equally active against replicating and non-replicating form of Mtb (MIC(MABA) 1.98 and 1.66 μg/ml; MIC(LORA) 2.06 and 1.59 μg/ml respectively). They arrested the cell division (replicating Mtb) by inhibiting the GTPase activity of FtsZ with IC50 values 45 and 64 μM respectively. They were also capable of kill Mtb in non-replicating form by inhibiting the biosynthesis of menaquinone which was substantiated by the MenG inhibition (IC50 = 11.62 and 7.49 μM respectively) followed by the Vit-K2 rescue study and ATP production assay.
- Datta, Dhrubajyoti,Debnath, Joy,Franzblau, Scott G.,Ghosh, Kalyan Sundar,Hari, Natarajan,Ma, Rui,Rana, Shiwani,Velappan, Anand Babu
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- Small molecule inhibition of microRNA-21 expression reduces cell viability and microtumor formation
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MicroRNAs (miRNAs) are short, non-coding RNA molecules estimated to regulate expression of a large number of protein-coding genes and are implicated in a variety of biological processes such as development, differentiation, proliferation, and cell surviva
- Ankenbruck, Nicholas,Kumbhare, Rohan,Naro, Yuta,Thomas, Meryl,Gardner, Laura,Emanuelson, Cole,Deiters, Alexander
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supporting information
p. 3735 - 3743
(2019/07/03)
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- Tribenzazole amine derivatives and organic electroluminescent device including the same
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The present invention provides a tribenzazole amine derivative which contributes to substantial life improvement of an organic electroluminescent device by effectively absorbing a high energy external light source of an UV area and minimizing the damage of organic materials in the organic electroluminescent device. The organic electroluminescent device according to the present invention includes: a first electrode; a second electrode; an organic material layer disposed between the first electrode and the second electrode; and a capping layer disposed on the second electrode. The capping layer includes a tribenzazole amine derivative represented by chemical formula 1. In chemical formula 1, R^1, R^2 and R^3 are the same as or different from each other and are respectively and independently hydrogen and an alkyl group having 1 to 10 carbon atoms. l, n, and m are integers of 0 to 4.COPYRIGHT KIPO 2020
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- Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition
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Structure based virtual screening attempts to discover DUSP1 inhibitors have yielded a scaffold featuring benzoxazole and acylthiourea pharmacophore. A series of its analogues were synthesized to explore structure activity relationship (SAR) of DUSP1 inhi
- Yeon Kim, Bo,Hee Yoon, Ji,Kim, Myeongbin,Nyoung Kim, Jae,Park, Hwangseo,Eon Ryu, Seong,Lee, Sangku
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p. 1746 - 1748
(2019/05/21)
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- Synthesis and characterization of a novel oxo-bridged binuclear iron(iii) complex: Its catalytic application in the synthesis of benzoxazoles using benzyl alcohol in water
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In the present work, the synthesis and characterization of a novel binuclear oxo-bridged iron(iii) complex, (FeLAPIP)2O, where LAPIP is the deprotonated form of a tetradentateo-aminophenol-iminopyridine ligand, is described. The iron complex was characterized using different techniques including X-ray crystallography, infrared spectroscopy, UV-Vis, magnetic susceptibility and cyclic voltammetry. The X-ray structure analysis revealed that in the structure of the (FeLAPIP)2O complex, each iron(iii) is coordinated in a distorted square pyramidal arrangement by an oxo group, three amine nitrogens and one oxygen atom of the o-aminophenolate ligand. The variable-temperature magnetic measurement exhibits strong antiferromagnetic coupling between two iron(iii) centers. Cyclic voltammetry measurements showed two kinds of quasireversible events, suggesting the formation of a phenoxyl radical species in the region of the anodic peaks and a metal-centered redox (FeIII/FeII) process at low potential. The catalytic activity of this Fe-complex was evaluated in coupling of 2-aminophenol and benzyl alcohols for the one-pot synthesis of benzoxazoles. The catalyst system showed high catalytic activity in this transformation and benzoxazole derivatives were obtained in good to excellent yields. tert-Butyl hydroperoxide was used as an oxidant and 1.2 mol% of catalyst was needed to accomplish the reaction in water as the green solvent.
- Safaei, Elham,Alaji, Zahra,Panahi, Farhad,Wojtczak, Andrzej,Jagli?i?, Janez Zvonko
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supporting information
p. 7230 - 7236
(2018/05/07)
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- Ruthenium-catalyzed synthesis of benzoxazoles using acceptorless dehydrogenative coupling reaction of primary alcohols with 2-aminophenol under heterogeneous conditions
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An efficient ruthenium-catalyzed acceptorless dehydrogenative coupling reaction of primary alcohols with 2-aminophenol for one-pot synthesis of benzoxazoles is introduced. The phosphine-functionalized magnetic nanoparticles (PFMNPs; Fe3O4@SiO2@PPh2) as a magnetic recyclable phosphorus ligand in the presence of Ru2Cl 4(CO)6 was found to be an efficient heterogeneous catalytic system for promotion of the designed protocol. The reaction was carried out efficiently with a variety of substrates to give the corresponding products in moderate to good yields.
- Khalafi-Nezhad, Ali,Panahi, Farhad
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p. 1686 - 1692
(2014/06/24)
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- Synthesis and antibacterial evaluation of benzazoles tethered dihydro[1,3]oxazines
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Synthesis of various benzazoles tethered 1,3-oxazines such as 1H-benzo[d]azolophenyl-3,4-dihydro-2H-benzo- [e][1,3]oxazines 2a-j, 2-(3-(1H-benzo[d]oxazol-2-yl)phenyl)-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine 3, 2-(3-(1Hbenzo-[ d]imidazol-2-yl)phenyl)-2,3
- Prasada, Davinder,Kumar Rohilla, Rajesh,Roy, Nilanjan,Nath, Mahendra
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p. 739 - 745
(2012/07/01)
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- Design and synthesis of 2-arylbenzimidazoles and evaluation of their inhibitory effect against Chlamydia pneumoniae
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Chlamydia pneumoniae is an intracellular bacterium that responds poorly to antibiotic treatment. Insufficient antibiotic usage leads to chronic infection, which is linked to disease processes of asthma, atherosclerosis, and Alzheimer's disease. The Chlamydia research lacks genetic tools exploited by other antimicrobial research, and thus other approaches to drug discovery must be applied. A set of 2-arylbenzimidazoles was designed based on our earlier findings, and 33 derivatives were synthesized. Derivatives were assayed against C. pneumoniae strain CWL-029 in an acute infection model using TR-FIA method at a concentration of 10 μM, and the effects of the derivatives on the host cell viability were evaluated at the same concentration. Fourteen compounds showed at least 80% inhibition, with only minor changes in host cell viability. Nine most potential compounds were evaluated using immunofluorescence microscopy on two different strains of C. pneumoniae CWL-029 and CV-6. The N-[3-(1H-benzimidazol-2-yl)phenyl]-3-methylbenzamide (42) had minimal inhibitory concentration (MIC) of 10 μM against CWL-029 and 6.3 μM against the clinical strain CV-6. This study shows the high antichlamydial potential of 2-arylbenzimidazoles, which also seem to have good characteristics for lead compounds.
- Keurulainen, Leena,Salin, Olli,Siiskonen, Antti,Kern, Jan Marco,Alvesalo, Joni,Kiuru, Paula,Maass, Matthias,Yli-Kauhaluoma, Jari,Vuorela, Pia
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p. 7664 - 7674
(2011/03/17)
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- ANTIBACTERIAL AGENTS
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The application concerns compounds for use as antibacterial agents, processes for their preparation, and compositions comprising said agents, wherein said compounds have formula (VI) and r, p, R1, R2, R3 and R4
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Page/Page column 36
(2009/07/25)
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- SUBSTITUTED PHENYLUREA DERIVATIVES AS HDAC INHIBITORS
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A series of phenylurea derivatives, further substituted on the phenyl ring by a benzoxazole, benzothiazole or benzimidazole moiety, being inhibitors of histone deacetylase, are accordingly of use in medicine, in particular for the treatment of cancer.
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- 2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: A novel class of small molecule heparanase inhibitors
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A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids are described as inhibitors of the endo-β-glucuronidase heparanase. Several of the compounds, for example, 2-[4-propylamino-5-[5-(4-chloro)phenyl-benzoxazol-2- yl]phenyl]-2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid (9c), display potent heparanase inhibitory activity (IC50 200-500nM) and have high selectivity (>100-fold) over human β-glucuronidase. They also show anti-angiogenic effects. Such compounds should serve as useful biological tools and may provide a basis for the design of novel therapeutic agents.
- Courtney, Stephen M.,Hay, Philip A.,Buck, Richard T.,Colville, Claire S.,Porter, David W.,Scopes, David I. C.,Pollard, Faye C.,Page, Martin J.,Bennett, James M.,Hircock, Margaret L.,McKenzie, Edward A.,Stubberfield, Colin R.,Turner, Paul R.
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p. 3269 - 3273
(2007/10/03)
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- PHTHALIMIDE CARBOXYLIC ACID DERIVATIVES
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The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II). R is hydrogen, C1-C6 alkyl, aryl or C1-C3 alkylaryl and R2, R3 and R4 represent various substituents.
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Page/Page column 14-15
(2008/06/13)
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