925252-77-3Relevant academic research and scientific papers
Nitrobenzofurazan derivatives of N′-hydroxyamidines as potent inhibitors of indoleamine-2,3-dioxygenase 1
Paul, Saurav,Roy, Ashalata,Deka, Suman Jyoti,Panda, Subhankar,Trivedi, Vishal,Manna, Debasis
, p. 364 - 375 (2016/06/13)
Tryptophan metabolism through the kynurenine pathway is considered as a crucial mechanism in immune tolerance. Indoleamine 2,3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism in the immune system and it is also considered as an important therapeutic target for the treatment of cancer and other diseases that are linked with kynurenine pathway. In this study, a series of nitrobenzofurazan derivatives of N′-hydroxybenzimidamides (1) and N′-hydroxy-2-phenylacetimidamides (2) were synthesized and their inhibitory activities against human IDO1 enzyme were tested using in-vitro and cellular enzyme activity assay. The optimization leads to the identification of potent compounds, 1d, 2i and 2k (IC50 = 39-80 nM), which are either competitive or uncompetitive inhibitors of IDO1 enzyme. These compounds also showed IDO1 inhibition potencies in the nanomolar range (IC50 = 50-71 nM) in MDA-MB-231 cells with no/negligible amount of cytotoxicity. The stronger selectivity of the potent compounds for IDO1 enzyme over tryptophan 2,3-dioxygenase (TDO) enzyme (312-1593-fold) also makes them very attractive for further immunotherapeutic applications.
Novel benzimidazole-oxadiazole hybrid molecules as promising antimicrobial agents
Shruthi,Poojary, Boja,Kumar, Vasantha,Hussain, Mumtaz Mohammed,Rai, Vaishali M.,Pai, Vinitha R.,Bhat, Mahima,Revannasiddappa
, p. 8303 - 8316 (2016/02/09)
In the present study, we describe the design and expeditious synthesis of novel 2-aryl-5-(3-aryl-[1,2,4]-oxadiazol-5-yl)-1-methyl-1H-benzo[d]imidazole hybrid molecules as promising antimicrobial agents. The core moiety 2-aryl-ethyl-1H-benzo[d]imidazole-5-
Molecular properties prediction and synthesis of new oxadiazole derivatives possessing 3-fluoro-4-methoxyphenyl moiety as potent anti-inflammatory and analgesic agents
Dinesha,Viveka, Shivapura,Khandige, Prasanna S.,Nagaraja, Gundibasappa K.
, p. 435 - 443 (2016/02/16)
A new series of 1,2,4- and 1,3,4-oxadiazole derivatives possessing 3-fluoro-4-methoxyphenyl moiety were efficiently synthesized and characterized by spectroscopic methods and elemental analysis. All the compounds were evaluated in vivo for their anti-infl
Synthesis, Crystal Structure, and Characterization of (Z) -2-(3-chlorophenyl)- N -hydroxyacetamidine
Prabhuswamy,Dinesha,Abdoh,Pampa,Madan Kumar,Nagaraja,Lokanath
, p. 189 - 198 (2015/11/02)
The compound (Z)-2-(3-chlorophenyl)-N-hydroxyacetamidine, (2) was synthesized and characterized by 1H NMR, FT-IR, TGA, UV-Visible Spectra, and elemental analysis. Its molecular structure was solved by single-crystal X-ray diffraction method. Th
OXADIAZOLE COMPOUNDS
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Page/Page column 143; 144, (2015/11/11)
The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1,R2,R3,L1,L2,L3,L4,L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP)
Rackham, Mark D.,Brannigan, James A.,Rangachari, Kaveri,Meister, Stephan,Wilkinson, Anthony J.,Holder, Anthony A.,Leatherbarrow, Robin J.,Tate, Edward W.
supporting information, p. 2773 - 2788 (2014/04/17)
N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4-yloxy)benzo[b]thiophen-2-yl)-5-((1,3, 5-trimethyl-1H-pyrazol-4-yl)meth
NOVEL COMPOUNDS AND THEIR USE IN THERAPY
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Page/Page column 90; 100; 101-102, (2013/06/27)
The invention provides compounds which inhibit N-myristoyltransferase and are selective for protozoal N-myristoyltransferase and, consequently suitable to treat microbial infections, including viral and fungal infections, and protozoan infections such as malaria, leishmaniasis and sleeping sickness.
Aryl and heteroaryl alkoxynaphthalene derivatives
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, (2008/06/13)
Compounds of the formula wherein R1, R2, R4, R23, R24, R25 and R26 are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists.
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70
Vu, Chi B.,Corpuz, Evelyn G.,Merry, Taylor J.,Pradeepan, Selvaluxmi G.,Bartlett, Catherine,Bohacek, Regine S.,Botfield, Martyn C.,Eyermann, Charles J.,Lynch, Berkley A.,MacNeil, Ian A.,Ram, Mary K.,Van Schravendijk, Marie Rose,Violette, Shelia,Sawyer, Tomi K.
, p. 4088 - 4098 (2007/10/03)
A series of 1,2,4-oxadiazole analogues has been shown to be potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70, a potential therapeutic target for immune suppression. These compounds typically are 200- 400-fold more potent than the native,
Use of naphthalene derivatives in treating lung carcinoma
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, (2008/06/13)
A method of inhibiting cell growth in human small cell lung carcinoma comprising administering to a mammal in need of such treatment a cell growth inhibitory amount of a compound of the formula STR1
