- Synthesis and comprehensive structural studies of a novel amide based carboxylic acid derivative: Non–covalent interactions
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The presented work studies the geometric and electronic structures of the crystalline network of a novel amide based carboxylic acid derivative, N–[(4–chlorophenyl)]–4–oxo–4–[oxy] butane amide, C10H10NO3Cl (1), constructed
- Chahkandi, Mohammad,Bhatti, Moazzam H.,Yunus, Uzma,Shaheen, Shahida,Nadeem, Muhammad,Tahir, Muhammad Nawaz
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- Design, synthesis and biological evaluation of anilide (dicarboxylic acid) shikonin esters as antitumor agents through targeting PI3K/Akt/mTOR signaling pathway
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Triple-negative breast cancer (TNBC) has an unfavorable prognosis attribute to its low differentiation, rapid proliferation and high distant metastasis rate. PI3K/Akt/mTOR as an intracellular signaling pathway plays a key role in the cell proliferation, m
- Ma, Yingying,Yang, Xiaorong,Han, Hongwei,Wen, Zhongling,Yang, Minkai,Zhang, Yahan,Fu, Jiangyan,Wang, Xuan,Yin, Tongming,Lu, Guihua,Qi, Jinliang,Lin, Hongyan,Wang, Xiaoming,Yang, Yonghua
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- Identification of two arylimides as cholinesterase inhibitors and testing of propranolol addition on impaired rat memory
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Alzheimer's disease (AD) is clearly linked to the decline of acetylcholine (ACh) effects in the brain. These effects are regulated by the hydrolytic action of acetylcholinesterase (AChE). Therefore, a central palliative treatment of AD is the administration of AChE inhibitors although additional mechanisms are currently described and tested for generating advantageous therapeutic strategies. In this work, we tested new arylamides and arylimides as potential inhibitors of AChE using in silico tools. Then, these compounds were tested in vitro, and two selected compounds, C7 and C8, as well as propranolol showed inhibition of AChE. In addition, they demonstrated an advantageous acute toxicity profile compared to that of galantamine as a reference AChE inhibitor. in vivo evaluation of memory performance enhancement was performed in an animal model of cognitive disturbance with each of these compounds and propranolol individually as well as each compound combined with propranolol. Memory improvement was observed in each case, but without a significant additive effect with the combinations.
- Ciprés-Flores, Fabiola J.,Farfán-García, Eunice D.,Andrade-Jorge, Erik,Cuevas-Hernández, Roberto I.,Tamay-Cach, Feliciano,Martínez-Archundia, Marlet,Trujillo-Ferrara, José G.,Soriano-Ursúa, Marvin A.
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p. 256 - 266
(2019/12/30)
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- An expeditious synthesis of imides from phthalic, maleic and succinic anhydrides and chemoselective C=C reduction of maleic amide esters
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Phthalic, maleic and succinic anhydrides have been reacted with aromatic amines to obtain the corresponding monoacid monoamides. The latter have been each transformed into the corresponding cyclic imide derivatives by treating with SOCl2. Alternatively, anhydrides have been reacted with methanolic KOH to obtain monomethyl ester derivatives which on reaction with aromatic amines in the presence of EDC. HCl and HOBt give cyclic imide derivatives. Reaction of monoacid monoamides independently, with SOCl 2 at 0-5°C give the monoamide monoester derivatives. Treatment of monoamide monoester of malic anhydride with NaBH4 leads to the unusual reduction of C=C grouping as well as the carbonyl group of the ester group to from monoamide monoalcohol of succinic anhydride. Preparation of monoamide monoalcohol of succinic anhydride can also be achieved by chemoselective reduction of monoamide monoester of malic anhydride with Mg turnings yielding monoamide monoester of succinic anhydride followed by reduction of the latter with NaBH4.
- Kumar, Padam Praveen,Reddy, Y. Dathu,Kumari, Y. Bharathi,Devi, B. Rama,Dubey
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p. 392 - 398
(2014/05/06)
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- A facile and green synthesis of N-substituted imides
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Anhydrides 1, 6 and 10 have been reacted, independently, with aromatic primary amines 2 in solid phase by simple physical grinding of reactants with p-toluenesulphonicacid as a catalyst to yield corresponding open chain derivatives, monoacid monoamides3,7 and 11 respectively. The latter have each been transformed into the corresponding cyclic derivatives, i.e. imides 5, 9 and 13 respectively in solid phase by simple physical grinding of each with K 2CO3, alkylating agent and tetrabutylammoniumbromide as a catalyst with short reaction times. These cyclic imides can also be obtained by physical grinding of each of 3, 7 and 11 with dicyclohexylcarbodimide as a dehydrating agent in solid phase.
- Kumar, Padam Praveen,Rama Devi,Dubey
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p. 1166 - 1171
(2013/09/24)
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- HIV INHIBITORS
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Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
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Paragraph 0290
(2013/03/26)
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- Synthesis of the major metabolites of Tolvaptan
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Tolvaptan is a nonpeptide arginine vasopressin (AVP) V2-receptor antagonist and used in the treatment of heart failure, cirrhosis, syndrome of inappropriate antidiuretic hormone secretion or other high-volume capacity of hyponatremia. The metab
- Wan, Wei Li,Wu, Jian Bo,Lei, Fan,Li, Xiao Long,Hai, Li,Wu, Yong
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p. 1343 - 1346
(2013/02/22)
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- Design, synthesis, and antiviral activity of entry inhibitors that target the CD4-binding site of HIV-1
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The CD4 binding site on HIV-1 gp120 has been validated as a drug target to prevent HIV-1 entry to cells. Previously, we identified two small molecule inhibitors consisting of a 2,2,6,6-tetramethylpiperidine ring linked by an oxalamide to a p-halide-substituted phenyl group, which target this site, specifically, a cavity termed "Phe43 cavity". Here we use synthetic chemistry, functional assessment, and structure-based analysis to explore variants of each region of these inhibitors for improved antiviral properties. Alterations of the phenyl group and of the oxalamide linker indicated that these regions were close to optimal in the original lead compounds. Design of a series of compounds, where the tetramethylpiperidine ring was replaced with new scaffolds, led to improved antiviral activity. These new scaffolds provide insight into the surface chemistry at the entrance of the cavity and offer additional opportunities by which to optimize further these potential-next- generation therapeutics and microbicides against HIV-1.
- Curreli, Francesca,Choudhury, Spreeha,Pyatkin, Ilya,Zagorodnikov, Victor P.,Bulay, Anna Khulianova,Altieri, Andrea,Kwon, Young Do,Kwong, Peter D.,Debnath, Asim K.
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supporting information; experimental part
p. 4764 - 4775
(2012/07/28)
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- Bicyclic guanidine-catalyzed direct asymmetric allylic addition of N-aryl alkylidene-succinimides
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Enantio-enriched maleimides and succinimides that can be used to prepare aza-heterocycles with multiple chiral centers are obtained from the bicyclic guanidine-catalyzed direct asymmetric allylic addition of N-aryl alkylidene-succinimides to imines. NMR studies and deuterium-exchange experiments were used to study the intermediates in the reaction.
- Wang, Jianmin,Liu, Hongjun,Fan, Yitian,Yang, Yuanyong,Jiang, Zhiyong,Tan, Choon-Hong
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supporting information; experimental part
p. 12534 - 12537
(2011/02/22)
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- Solid-phase synthesis of N-aryl succinimides
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A new method upon adopting a solid-phase strategy for synthesis of N-aryl succinimides is described here, using the silica-bound benzoyl chloride (SBBC) as dehydrating agent in reaction with N-arylsuccinamic acids. The main advantage of this method is the
- Rad-Moghadam, Kurosh,Kheyrkhah, Leila
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experimental part
p. 2108 - 2115
(2009/10/17)
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- Substituent chemical shifts of N-arylsuccinanilic acids, N-arylsuccinimides, N-arylmaleanilic acids, and N-arylmaleimides
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NMR spectra of a series of N-arylsuccinanilic acids, N-arylsuccinimides, N-arylmaleanilic acids, and N-arylmaleimides were examined to estimate the electronic effect of the amide and imide groups on the chemical shifts of the hydrogen and carbon nuclei of the benzene ring.
- Lee, Hye Sun,Yu, Ji Sook,Lee, Chang Kiu
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scheme or table
p. 711 - 715
(2010/07/05)
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- Hydroxamic Acid Production by α-Ketoglutarate Dehydrogenase. Part 2. Evidence for an Electrophilic Reaction Intermediate at the Enzyme Active Site
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The α-ketoglutarate dehydrogenase-catalysed conversion of 4-chloronitrosobenzene (1) into the hydroxamic acid (3) and the Bamberger-rearrangement product (6) was investigated by use of radiotracer methods and nucleophilic trapping agents. 14C-Labelled 4-c
- Corbett, Michael D.,Doerge, Daniel R.,Corbett, Bernadette R.
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p. 765 - 770
(2007/10/02)
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