5180-75-6Relevant academic research and scientific papers
Design and development of novel p-aminobenzoic acid derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease
Shrivastava, Sushant K.,Sinha, Saurabh K.,Srivastava, Pavan,Tripathi, Prabhash N.,Sharma, Piyoosh,Tripathi, Manish K.,Tripathi, Avanish,Choubey, Priyanka K.,Waiker, Digambar K.,Aggarwal, Lalit M.,Dixit, Manish,Kheruka, Subhash C.,Gambhir, Sanjay,Shankar, Sharmila,Srivastava, Rakesh K.
, p. 211 - 223 (2019)
Based on the quantitative structure-activity relationship (QSAR), some novel p-aminobenzoic acid derivatives as promising cholinesterase enzyme inhibitors were designed, synthesized, characterized and evaluated to enhance learning and memory. The in vitro
Urethane hapten composition and artificial antigen composition, and preparation methods and application thereof
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Paragraph 0039; 0040, (2017/03/08)
The invention discloses a urethane hapten composition and artificial antigen composition, and preparation methods and application thereof. The urethane artificial antigen composition has molecular structures as shown in a formula (III) and a formula (IV).
Synthesis, analysis, cholinesterase-inhibiting activity and molecular modelling studies of 3-(dialkylamino)-2-hydroxypropyl 4-[(alkoxy-carbonyl)amino]benzoates and their quaternary ammonium salts
Padrtova, Tereza,Marvanova, Pavlina,Odehnalova, Klara,Kubinova, Renata,Parravicini, Oscar,Garro, Adriana,Enriz, Ricardo D.,Humpa, Otakar,Oravec, Michal,Mokry, Petr
, (2017/12/05)
Tertiary amines 3-(dialkylamino)-2-hydroxypropyl 4-[(alkoxycarbonyl)amino]benzoates and their quaternary ammonium salts were synthesized. The final step of synthesis of quaternary ammonium salts was carried out by microwave-assisted synthesis. Software-ca
An integrative study to identify novel scaffolds for sphingosine kinase 1 inhibitors
Vettorazzi, Marcela,Angelina, Emilio,Lima, Santiago,Gonec, Tomas,Otevrel, Jan,Marvanova, Pavlina,Padrtova, Tereza,Mokry, Petr,Bobal, Pavel,Acosta, Lina M.,Palma, Alirio,Cobo, Justo,Bobalova, Janette,Csollei, Jozef,Malik, Ivan,Alvarez, Sergio,Spiegel, Sarah,Jampilek, Josef,Enriz, Ricardo D.
, p. 461 - 481 (2017/08/21)
Sphingosine kinase 1 (SphK1), the enzyme that produces the bioactive sphingolipid metabolite, sphingosine-1-phosphate, is a promising new molecular target for therapeutic intervention in cancer and inflammatory diseases. In view of its importance, the main objective of this work was to find new and more potent inhibitors for this enzyme possessing different structural scaffolds than those of the known inhibitors. Our theoretical and experimental study has allowed us to identify two new structural scaffolds (three new compounds), which could be used as starting structures for the design and then the development of new inhibitors of SphK1. Our study was carried out in different steps: virtual screening, synthesis, bioassays and molecular modelling. From our results, we propose a new dihydrobenzo[b]pyrimido[5,4-f]azepine and two alkyl{3-/4-[1-hydroxy-2-(4-arylpiperazin-1-yl)ethyl]phenyl}carbamates as initial structures for the development of new inhibitors. In addition, our molecular modelling study using QTAIM calculations, allowed us to describe in detail the molecular interactions that stabilize the different Ligand-Receptor complexes. Such analyses indicate that the cationic head of the different compounds must be refined in order to obtain an increase in the binding affinity of these ligands.
Oxime-Based carbonates as useful reagents for both n-protection and peptide coupling
Jad, Yahya El-Sayed,Khattab, Sherine N.,El-Faham, Ayman,Albericio, Fernando
, p. 14361 - 14376 (2013/03/13)
We have demonstrated that oxime-based mixed carbonates are very effective reagents for both N-protection and peptide coupling.
A new access to quinazolines from simple anilines
Chilin, Adriana,Marzaro, Giovanni,Zanatta, Samuele,Barbieri, Vera,Pastorini, Giovanni,Manzini, Paolo,Guiotto, Adriano
, p. 12351 - 12356 (2007/10/03)
A new synthetic pathway to quinazolines is described. This new method uses hexamethylenetetramine in TFA and potassium ferricyanide in aqueous ethanolic KOH, starting from simple N-protected anilines. The method affords substituted quinazolines with high
Synthesis of some heterocycle containing urea derivatives and their anti-viral activity
Verma, Majusha,Singh, Krishna N.,Clercq, Erik D.
, p. 11 - 22 (2007/10/03)
Some new isoindol heterocyclic ureas (6a-6i) have been synthesized using N-aminophthalimide (2) and ethyl N-monosubstituted/ethyl N,N-disubstituted carbamate (5a-5i). All the newly synthesized final compounds have been evaluated for their anti-viral activities against a variety of viruses. The compound (6f) with the methoxy substituent showed reasonably better activity as compared to the standard drugs against all the viruses (cf. Tables 1, 2 and 3). Further, all the products (6a-6i) were found to be active against Vesicular stomatitis virus, Coxsackie virus B4 and Respiratory syncytical virus (cf. Table 2) and the compounds (6h) and (6i) displayed better antiviral activity in comparison to Brivudin and (S)-DHPA (cf. Table 3).
Synthesis and pharmacological evaluation of novel potential ultrashort-acting β-blockers
Mokry,Zemanova,Csoellei,Racanska,Tumova
, p. 18 - 21 (2007/10/03)
The basic relationship between chemical structure and pharmacological activity of eight newly developed potential ultrashort-acting β-adrenergic blockers was evaluated. The compounds studied are derivatives of arylcarbonyloxyaminopropanols and were prepar
