- Synthesis, characterization and docking studies of anti-HCV molecules
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The present study reports the synthesis and characterization of novel molecules inhibiting the spread of hepatitis C. The molecules were designed as to block the NS3/4A protease enzyme on HCV RNA. The molecules were synthesized using usual peptide synthesis techniques. Compounds with purity more than 95% were characterized and docking studies were also performed. All the compounds were characterized using physico-chemical techniques such as determination of melting point by DSC and NMR, mass, IR spectral studies. The docking studies were also conducted to assess the activity of molecules for inhibition of hepatitis C virus.
- Kumar, Satish,Santra,Dwivedi,Aryan
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p. 1221 - 1229
(2020/06/09)
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- Stereoselectivity and regioselectivity in nucleophilic ring opening in derivatives of 3-phenylisoxazolo[2,3-a]pyrimidine. Unpredicted dimerization and ring transformation. Syntheses of derivatives of pyrimidinylmethylamine, pyrimidinylmethylamino acid ami
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The nucleophilic ring opening of the isoxazolone ring in 2-oxo-3-phenylisoxazolo[2,3-a]pyrimidine derivatives by optically active amino acid amides and ephedrine led to pyrimidinylmethylamino acid amides. Using amides of different L-amino acids and (-)-ep
- Zvilichovsky, Gury,Gbara-Haj-Yahia, Isra
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p. 4966 - 4973
(2007/10/03)
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- A catalyst for asymmetric induction
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A catalyst for asymmetric induction is provided which comprises a titanium (IV) alkoxide and an amino acid amide derivative of formula (I): wherein R1 is isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl or benzyl, R2 and R3 are the same or different and each is lower alkyl, C3 to C8 cycloalkyl, unsubstituted or substituted phenyl or hydrogen or R2 and R3 together form a divalent C3 to C7 alkylene group optionally containing one or more hetero atoms, R4 is chlorine, bromine, iodine, lower alkyl or unsubstituted or substituted phenyl, R5, R6 and R7 are the same or different and each is hydrogen, halogen, methyl or methoxy or R5 is as defined above and R6 and R7 together form -CH=CH-CH=CH- or -OCH2O- or R7 is as defined above and R5 and R6 together form -CH=CH-CH=CH- or -OCH2O- and * denotes an absolute configuration of S or R.
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- Peptide-titanium complex as catalyst for asymmetric addition of hydrogen cyanide to aldehyde
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The complex of titanium ethoxide and an acyclic dipeptide ester whose terminal amino group is modified to a salicylal-type Schiff base catalyzes the asymmetric addition of hydrogen cyanide to aldehydes with high enantioselectivity. In the reaction of benzaldehyde and hydrogen cyanide, (R)-mandelonitrile is obtained with an enantiomeric excess of 90% when N-((2-hydroxy-1-naphthyl)methylene)-(S)-valyl-(S)-tryptophan methyl ester is employed. In place of the dipeptide, the amide derivatives of an amino acid modified by substituted salicylaldehyde, such as N-(3,5-dibromosalicylidene)-(S)-valine piperidide, exhibit an entirely opposite stereoselectivity to yield S-cyanohydrins with optical purities up to 97% ee. This novel peptide-titanium complex, therefore, enables us to afford optically active cyanohydrins of both absolute configurations by using natural S-amino acids as chiral auxiliaries.
- Nitta, Hideaki,Yu, Donghai,Kudo, Masanobu,Mori, Atsunori,Inoue, Shohei
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p. 7969 - 7975
(2007/10/02)
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