163959-79-3Relevant articles and documents
PF74 and its novel derivatives stabilize hexameric lattice of HIV-1 mature-like particles
?kach, Kry?tof,Dostálková, Al?běta,Flegel, Martin,Hadravová, Romana,Hrabal, Richard,K?í?ová, Ivana,Kaufman, Filip,Ruml, Tomá?,Rumlová, Michaela
, (2020/04/27)
A major structural retroviral protein, capsid protein (CA), is able to oligomerize into two different hexameric lattices, which makes this protein a key component for both the early and late stages of HIV-1 replication. During the late stage, the CA prote
Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents
Alasmary, Fatmah A.S.,Snelling, Anna M.,Zain, Mohammed E.,Alafeefy, Ahmed M.,Awaad, Amani S.,Karodia, Nazira
supporting information, p. 15206 - 15223 (2015/09/21)
A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1Hbenzo[ d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.
Asymmetric Hydrogenation of 3,5-Bistrifluoromethyl Acetophenone in Pilot Scale with Industrially Viable Ru/Diphosphine-Benzimidazole Complexes
Xu, Liang,Huang, Zhi-Hong,Sandoval, Christian A.,Gu, Lian-Quan,Huang, Zhi-Shu
, p. 1137 - 1141 (2015/04/22)
A novel efficient asymmetric hydrogenation (AH) process was developed for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethanol (3), using a catalyst Ru/(4R,5R)-(+)-4,5-bis(diphenylphosphinomethyl)-2,2-dimethyl-1,3-dioxoane-(R,R-Diop)-2R-(α-met
Stereoselective chemoenzymatic synthesis of enantiopure 1-(Heteroaryl)ethanamines by lipase-Catalysed kinetic resolutions
Alatorre-Santamaria, Sergio,Gotor-Fernandez, Vicente,Gotor, Vicente
experimental part, p. 2533 - 2538 (2009/09/25)
The efficient chemical synthesis and enzymatic kinetic resolution of a family of 1-(heteroaryl)ethanamines have been performed with lipases responsible for the preparation of nitrogenated compounds in high optical purity. Thus, Candida antarctica lipase type B has been identified as an excellent biocatalyst for the stereoselective production of the corresponding enantiomerically enriched (B)-acetamides and (S)-amines. A similar effect of the heteroatom in the cyclic ring has been observed in terms of reactivity and enantio- selectivity, with benzoxazole, benzothiazole and benzimidazole derivatives being obtained with excellent enantiopurities after one day of reaction. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009.
Hybrid NH2-benzimidazole ligands for efficient Ru-catalyzed asymmetric hydrogenation of aryl ketones
Li, Yuehui,Ding, Kuiling,Sandoval, Christian A.
supporting information; experimental part, p. 907 - 910 (2009/07/25)
Readily available hybrid NH2/benzimidazole ligands (R-bimaH, 1) dramatically influence the outcome of established Ru-based catalysts during asymmetric hydrogenation of aryl ketones. The benzimidazole functionality results in reversal of the typically observed chiral induction and allows for hydrogenation to be uncharacteristically conducted in nonprotic solvents. The developed systems efficiently catalyzed the AH of a number of ketones in up to 99% ee.
BENZIMIDAZOLE COMPOUNDS THAT ARE VITRONECTIN RECEPTOR ANTAGONISTS
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Page/Page column 31, (2008/06/13)
The present invention provides compounds having formula (I) wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y' each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, -CF3, and -C(O)OH; R, R, R and R are H or specified substituents; R, R, R, R, R, R, R and R are independently selected from H or C1-C3 alkyl; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.
Benzimidazole compounds that are vitronectin receptor antagonists
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, (2008/06/13)
The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d
Retroviral protease inhibitors
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, (2008/06/13)
Compounds of the formula I: STR1 wherein X, Y, Z, a, b, c, R1, R2, R3, R4 and R5 are defined in the specification are provided. The compounds are useful as inhibitors of retroviral protease enzymes.
Heterocyclization of the 2-aminoalkyl (and aryl) benzimidazoles under phase transfer catalysis conditions
Cherkaoui, O.,Essassi, E.M.,Zniber, R.
, p. 255 - 259 (2007/10/02)
A number of new imidazolo (pyrazino and diazepino) benzimidazoles have been prepared by reaction between 2-aminoalkyl (and aryl)benzimidazoles and dibromoalkanes Br-(CH2)n-Br under phase transfer catalysis conditions.These products have been characterized by 1H NMR, IR, MS and their microanalysis. --- Key words: heterocyclization / benzimidazole / diazepinobenzimidazole / benzimidazolo benzodiazepin
Search for non-steroidal anti-inflammatory agents. Part 1: Synthesis of 2-alkyl/aryl-3-benzimidazolylalkylquinazolon-4(3H)-ones.
Tiwari,Zaidi,Satsangi
, p. 73 - 75 (2007/10/02)
Sixteen title compounds have been synthesized and some of them have shown interesting results in antiinflammatory screening against carrageenin-induced inflammation. In addition, the compounds were found to be central nervous system depressants and relatively non-toxic.
