- Phenyl-oxamideHIV-1 inhibitors and preparation method and application thereof
-
The invention relates to phenyl-oxamideHIV-1 inhibitors and a preparation method and application thereof. Compounds have the structure shown in the formula I. The invention further relates to drug compositions containing the compounds with the structure s
- -
-
Paragraph 0023; 0036; 0038
(2019/07/04)
-
- Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase
-
In the last two decades, trans-sialidase of Trypanosoma cruzi (TcTS) has been an important pharmacological target for developing new anti-Chagas agents. In a continuous effort to discover new potential TcTS inhibitors, 3-amino-3-arylpropionic acid derivatives (series A) and novel phthaloyl derivatives (series B, C and D) were synthesized and molecular docking, TcTS enzyme inhibition and determination of trypanocidal activity were carried out. From four series obtained, compound D-11 had the highest binding affinity value (?11.1 kcal/mol) compared to reference DANA (?7.8 kcal/mol), a natural ligand for TS enzyme. Furthermore, the 3D and 2D interactions analysis of compound D-11 showed a hydrogen bond, π-π stacking, π-anion, hydrophobic and Van der Waals forces with all important amino acid residues (Arg35, Arg245, Arg314, Tyr119, Trp312, Tyr342, Glu230 and Asp59) on the active site of TcTS. Additionally, D-11 showed the highest TcTS enzyme inhibition (86.9% ± 5) by high-performance ion exchange chromatography (HPAEC). Finally, D-11 showed better trypanocidal activity than the reference drugs nifurtimox and benznidazole with an equal % lysis (63 ± 4 and 65 ± 2 at 10 μg/mL) and LC50 value (52.70 ± 2.70 μM and 46.19 ± 2.36 μM) on NINOA and INC-5 strains, respectively. Therefore, D-11 is a small-molecule with potent TcTS inhibition and a strong trypanocidal effect that could help in the development of new anti-Chagas agents.
- Kashif, Muhammad,Chacón-Vargas, Karla Fabiola,López-Cedillo, Julio Cesar,Nogueda-Torres, Benjamín,Paz-González, Alma D.,Ramírez-Moreno, Esther,Agusti, Rosalia,Uhrig, Maria Laura,Reyes-Arellano, Alicia,Peralta-Cruz, Javier,Ashfaq, Muhammad,Rivera, Gildardo
-
p. 252 - 268
(2018/07/14)
-
- β-alanine derivates
-
Alkanoic acid derivatives of formula (1) are described: [in-line-formulae]Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R??(1)[/in-line-formulae]Ar1 is an optionally subst
- -
-
Page/Page column 20
(2010/02/14)
-
- Enzymatic process for the enantiomeric resolution of amino acids
-
An enzymatic process permitting the enantiomeric resolution of amino acids is provided. More specifically, this process for separating the enantiomers of an amino acid comprises treating a racemic mixture of the amino acid with glutaric anhydride and then with the enzyme glutaryl-7-ACA acylase so as to recover one of the enantiomers of the amino acid, the other enantiomer remaining in the form of the corresponding glutarylamide derivative.
- -
-
-
- A one-pot synthesis of 3-amino-3-arylpropionic acids
-
3-Aminopropionic acids (β-amino acids) are biologically active compounds of interest in medicinal and pharmaceutical chemistry. Twenty-one 3-amino-3-arylpropionic acids were synthesized via a facile one-pot synthesis. In addition, a series of mechanistic studies have been performed to optimize the production of these β-amino acids. The reaction mechanism of this one-pot synthesis of β-amino acids, as well as the electronic effect of para-substitution and the influence of solvent polarity on the proposed reaction mechanism are discussed.
- Tan,Weaver
-
p. 7449 - 7461
(2007/10/03)
-
- Substituted aryl ureas as high potency sweeteners
-
Substituted ureas and thioureas are disclosed for use as high potency sweeteners.
- -
-
-