55477-81-1Relevant academic research and scientific papers
SUBSTITUTED HETEROCYCLICS WITH THERAPEUTIC ACTIVITY IN HIV
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Paragraph 0199-0200, (2021/05/29)
Substituted heterocyclic substituted pyrrole carboxamide compounds such as those represented by Formula I or Formula II are provided herein. Such compounds, or pharmaceutically acceptable salts thereof, can be used in the treatment of HIV infection and re
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation
Curreli, Francesca,Ahmed, Shahad,Benedict Victor, Sofia M.,Iusupov, Ildar R.,Belov, Dmitry S.,Markov, Pavel O.,Kurkin, Alexander V.,Altieri, Andrea,Debnath, Asim K.
, p. 1724 - 1749 (2020/03/10)
We previously reported a milestone in the optimization of NBD-11021, an HIV-1 gp120 antagonist, by developing a new and novel analogue, NBD-14189 (Ref1), which showed antiviral activity against HIV-1HXB2, with a half maximal inhibitory concentr
Synthesis of new β-amidodehydroaminobutyric acid derivatives and of new tyrosine derivatives using copper catalyzed C-N and C-O coupling reactions
Pereira,Vilaca,Ferreira
, p. 335 - 344 (2013/07/05)
Several β-amidodehydroaminobutyric acid derivatives were prepared from N,C-diprotected β-bromodehydroaminobutyric acids and amides by a copper catalyzed C-N coupling reaction. The best reaction conditions include the use of a catalytic amount of CuI, N,N'-dimethylethylenediamine as ligand and K 2CO3 as base in toluene at 110 C. The stereochemistry of the products was determined using NOE difference experiments and the results obtained are in agreement with an E-stereochemistry. Thus, the stereochemistry is maintained in the case of the E-isomers of β-bromodehydroaminobutyric acid derivatives, but when the Z-isomers were used as substrates the reaction proceeds with inversion of configuration. The use of β- bromodehydrodipeptides as substrates was also tested. It was found that the reaction outcome depend on the stereochemistry of the β- bromodehydrodipeptide and on the nature of the first amino acid residue. The products isolated were the β-amidodehydrodipeptide derivatives and/or the corresponding dihydropyrazines. The same catalytic system (CuI/N,N'- dimethylethylene diamine) was used in the C-O coupling reactions between a tyrosine derivative and aryl bromides. The new O-aryltyrosine derivatives were isolated in moderate to good yields. The photophysical properties of two of these compounds were studied in four solvents of different polarity. The results show that these compounds after deprotection can be used as fluorescence markers.
FIVE-MEMBERED HETEROCYCLIC DERIVATIVE
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Page/Page column 25, (2010/11/08)
The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.
Design and synthesis of carboxylate inhibitors for matrix metalloproteinases
Fujisawa,Katakura,Odake,Morita,Yasuda,Yasumatsu,Morikawa
, p. 1272 - 1279 (2007/10/03)
A series of carboxylate compounds were prepared from Nα-substituted 2,3-diaminopropionic acid and were tested for efficacy as matrix metalloproteinase (MMP) inhibitors. During modeling of the initial compound 10a, we utilized three-dimensional
Design and use of an oxazolidine silyl enol ether as a new homoalanine carbanion equivalent for the synthesis of carbon-linked isosteres of O- glycosyl serine and N-glycosyl asparagine
Dondoni, Alessandro,Marra, Alberto,Massi, Alessandro
, p. 933 - 944 (2007/10/03)
A trimethylsilyl enol ether carrying the N-Boc 2,2-dimethyloxazolidine ring was designed to serve as a synthetic equivalent of the homoalanine carbanion for the introduction of the α-amino acid side chain at the anomeric carbon of sugars. This new functio
DEHYDRATION OF β-HYDROXY-α-AMINO ACID DERIVATIVES WITH PHENYLTRIFLIMIDE
Torrini, Ines,Zecchini, Giampiero Pagani,Paradisi, Mario Paglialunga
, p. 695 - 704 (2007/10/02)
Conversion of N-protected β-hydroxy-α-amino esters to corresponding didehydroamino esters have been achieved using phenyltriflimide/triethylamine as a mild dehydrating agent.The selective formation of didehydroalanine derivatives from dipeptides containin
HOMOLYTIC DECARBOXYLATION OF GLUTAMATE ANALOGUES
Vidal-Cros, Anne,Bory, Sonia,Gaudry, Michel,Marquet, Andree
, p. 1799 - 1802 (2007/10/02)
The homolytic decarboxylation of a 3-cyclopropylglutamate derivative yields some rearrangement product whereas that of a 3-fluoroglutamate derivative yields the decarboxylation product without elimination.These results are discussed in relationship with t
