5933-35-7Relevant academic research and scientific papers
Axially Chiral Trifluoromethylbenzimidazolylbenzoic Acid: A Chiral Derivatizing Agent for α-Chiral Primary Amines and Secondary Alcohols to Determine the Absolute Configuration
Kriegelstein, Michal,Profous, David,Ly?ka, Antonín,Trávní?ek, Zdeněk,P?ibylka, Adam,Volná, Tereza,Benická, Sandra,Canka?, Petr
, p. 11911 - 11921 (2019/10/02)
Racemic 2-(2-trifluoromethyl)-1H-benzo[d]imidazol-1-yl)benzoic acid (TBBA) was synthesized in three steps from 1-fluoro-2-nitrobenzene. Target (P)- and (M)-TBBA atropisomers were stable with a racemization barrier above 30 kcal/mol. As a chiral derivatizi
Zn2+ mediated solvent free solid state red emitting fluorescent complex formation in a mortar-pestle along with living cell imaging studies
Adhikari, Susanta,Ghosh, Avijit,Mandal, Sandip,Sahana, Animesh,Das, Debasis
, p. 33878 - 33884 (2015/04/27)
An acridone based highly Zn2+ selective, cell-permeable turn-on fluorescence probe (AAS) shows yellow fluorescence at 560 nm (λex, 445 nm) in dry methanol/DMSO up to 100 μM Zn2+. At higher Zn2+ concentration (>1
The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs
Chen, Xin,Choo, Hyunah,Huang, Xi-Ping,Yang, Xiaobao,Stone, Orrin,Roth, Bryan L.,Jin, Jian
, p. 476 - 484 (2015/03/30)
Over the past decade, two independent technologies have emerged and been widely adopted by the neuroscience community for remotely controlling neuronal activity: optogenetics which utilize engineered channelrhodopsin and other opsins, and chemogenetics which utilize engineered G protein-coupled receptors (Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)) and other orthologous ligand-receptor pairs. Using directed molecular evolution, two types of DREADDs derived from human muscarinic acetylcholine receptors have been developed: hM3Dq which activates neuronal firing, and hM4Di which inhibits neuronal firing. Importantly, these DREADDs were not activated by the native ligand acetylcholine (ACh), but selectively activated by clozapine N-oxide (CNO), a pharmacologically inert ligand. CNO has been used extensively in rodent models to activate DREADDs, and although CNO is not subject to significant metabolic transformation in mice, a small fraction of CNO is apparently metabolized to clozapine in humans and guinea pigs, lessening the translational potential of DREADDs. To effectively translate the DREADD technology, the next generation of DREADD agonists are needed and a thorough understanding of structure-activity relationships (SARs) of DREADDs is required for developing such ligands. We therefore conducted the first SAR studies of hM3Dq. We explored multiple regions of the scaffold represented by CNO, identified interesting SAR trends, and discovered several compounds that are very potent hM3Dq agonists but do not activate the native human M3 receptor (hM3). We also discovered that the approved drug perlapine is a novel hM3Dq agonist with >10000-fold selectivity for hM3Dq over hM3.
Design, synthesis and anticancer activity evaluation of diazepinomicin derivatives
Yu, Yongguo,Wu, Jianbo,Lei, Fan,Chen, Lei,Wan, Weili,Hai, Li,Guan, Mei,Wu, Yong
, p. 369 - 373 (2013/07/26)
A series of diazepinomicin derivatives were synthesized and evaluated in vitro for their growth inhibitory activity against the human carcinoma cell lines. The results indicated the anticancer selectivity of this kind of compounds. Based on the results, preliminary structure-activity relationships were discussed.
Synthesis and characterization of 1-carboxyphenothiazine derivatives bearing nitrogen mustard as promising class of antitubercular agents
Kataria,Solanki,Trivedi,Shah
, p. 951 - 956 (2013/12/04)
A series of 1-carboxyphenothiazines bearing nitrogen mustard was synthesized, characterized, and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The results showed that compounds 5h, 5i and 5j found most active with percentage inhibition of 96, 91, and 92, respectively, at minimum inhibitory concentration (MIC) of 6.25 μg/mL. The structures of synthesized compounds were elucidated by various spectroscopic tools like IR, 1H NMR, 13C NMR, mass and elemental analysis. 2013 Bentham Science Publishers.
Synthesis of 11-(Piperazin-1-yl)-5H-dibenzo[b,e] [1,4]diazepine on kilo scale
Kalhapure, Rahul S.,Patil, Bhushan P.,Jadhav, Mahantesh N.,Kawle, Laxmikant A.,Wagh, Sanjay B.
experimental part, p. 1747 - 1749 (2012/05/07)
A synthesis of 11-(piperazin-1yl)-5H-dibenzo[b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization. Copyright E-Journal o
BENZIMIDAZOLONE CHYMASE INHIBITORS
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Page/Page column 224, (2009/01/20)
Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
N-Hydroxyamides Omege-Substituted with Tricyclic Groups as Histone Deacetylase Inhibitors, Their Preparation and Use in Pharmaceutical Formulations
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Page/Page column 3, (2008/12/08)
New N-hydroxyamides of n-alkyl carboxylic acids omega substituted with suitable tricyclic systems characterised by a central 7-membered ring, having activity as inhibitors of histone deacetylase (HDAC).
IRON CATALYZED CROSS-COUPLING REACTIONS OF IMIDOYL DERIVATIVES
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Page/Page column 18; 49, (2010/11/27)
Disclosed is a process for preparing a compound of formula A - N=C(D)(B), from a compound of formula A-N=C(E)(B) and a compound of formula D-M using an iron catalyst, where the process has is represented by Equation (I).
A simple and environmentally friendly method for the synthesis of N-phenylanthranilic acid derivatives
Girisha, Hanakere R.,Srinivasa, Gejjalagere R.,Gowda, D. Channe
, p. 342 - 344 (2007/10/03)
A simple, efficient and environmentally friendly method for the synthesis of N-phenylanthranilic acid derivatives by the copper acetate catalysed reaction of o-halobenzoic acid with anilines using sodium acetate as base and water as media is described.
