41373-36-8Relevant articles and documents
New pyrimidine-benzoxazole/benzimidazole hybrids: Synthesis, antioxidant, cytotoxic activity, in vitro cyclooxygenase and phospholipase A2-V inhibition
Abdelgawad, Mohamed A.,Bakr, Rania B.,Ahmad, Waqas,Al-Sanea, Mohammad M.,Elshemy, Heba A.H.
, (2019)
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
Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors
Malapati, Prasanthi,Krishna, Vagolu Siva,Nallangi, Radhika,Srilakshmi, Rudraraju Reshma,Sriram, Dharmarajan
, p. 23 - 34 (2018)
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
Discovery and computational studies of 2-phenyl-benzoxazole acetamide derivatives as promising P2Y14R antagonists with anti-gout potential
Zhou, Mengze,Wang, Weiwei,Wang, Zhongkui,Wang, Yilin,Zhu, Yifan,Lin, Zhiqian,Tian, Sheng,Huang, Yuan,Hu, Qinghua,Li, Huanqiu
, (2021/10/25)
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
A Diverse Range of Hemozoin Inhibiting Scaffolds Act on Plasmodium falciparum as Heme Complexes
Openshaw, Roxanne,Maepa, Keletso,Benjamin, Stefan J.,Wainwright, Lauren,Combrinck, Jill M.,Hunter, Roger,Egan, Timothy J.
, p. 362 - 376 (2021/02/01)
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.
Novel Phenolic Compounds as Potential Dual EGFR and COX-2 Inhibitors: Design, Semisynthesis, in vitro Biological Evaluation and in silico Insights
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.
, p. 2325 - 2337 (2022/01/13)
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
2-Aryl benzazole derived new class of anti-tubercular compounds: Endowed to eradicate mycobacterium tuberculosis in replicating and non-replicating forms
Datta, Dhrubajyoti,Debnath, Joy,Franzblau, Scott G.,Ghosh, Kalyan Sundar,Hari, Natarajan,Ma, Rui,Rana, Shiwani,Velappan, Anand Babu
, (2020/09/04)
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.
Benzoxazole derivative as well as preparation method and application thereof (by machine translation)
-
Paragraph 0029-0033, (2020/03/29)
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
Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition
Yeon Kim, Bo,Hee Yoon, Ji,Kim, Myeongbin,Nyoung Kim, Jae,Park, Hwangseo,Eon Ryu, Seong,Lee, Sangku
, p. 1746 - 1748 (2019/05/21)
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
Tribenzazole amine derivatives and organic electroluminescent device including the same
-
, (2020/01/31)
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
Small molecule inhibition of microRNA-21 expression reduces cell viability and microtumor formation
Ankenbruck, Nicholas,Kumbhare, Rohan,Naro, Yuta,Thomas, Meryl,Gardner, Laura,Emanuelson, Cole,Deiters, Alexander
supporting information, p. 3735 - 3743 (2019/07/03)
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
