106352-01-6Relevant academic research and scientific papers
Design and synthesis of a biologically active antibody mimic based on an antibody-antigen crystal structure
Smythe,Von Itzstein
, p. 2725 - 2733 (1994)
We have used the crystal structure of an N9 sialidase (antigen)-NC41 (antibody) complex to design a low molecular weight compound that mimics the binding function of the macromolecular antibody. The components of recognition between the antibody and the protein antigen have been analyzed from the energy-refined crystal complex. From this analysis, four amino acid residues on the antibody binding surface, which make direct contact with the active-site loop 368-370 of the antigen, have been identified as contributing the majority of the binding energy of the protein. The designed target compound, a constrained cyclic peptide, which mimics the receptor-bound conformation of these amino acids, has been synthesized and found to inhibit N9 sialidase activity, with a K(i) of 1 x 10-4 M.
ANTIBACTERIAL AGENTS
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Page/Page column 37, (2009/07/25)
The application concerns compounds for use as antibacterial agents, processes for their preparation, and compositions comprising said agents, wherein said compounds have formula (VI) and r, p, R1, R2, R3 and R4
Synthesis, characterization and biological activity of 1,3,4-substituted 2-azetidinones
Pandey,Gupta,Upadhyay, Mrinalini,Upadhyay, Mridula,Singh,Tandon, Meenal
, p. 158 - 162 (2007/10/03)
Amido/imido alcohol/2-phenyl-3-hydroxyethylquinazolin-4 (3H) -one 1 on treatment with benzoic acid in the presence of cone. H2SO4 yields m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxoquinazolinyl) benzoic acids 2. The acid chloride of 2 on reaction with hydrazine hydrate affords m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo-quinazolinyl) benzoic acid hydrazides 4 which on condensation with an aromatic aldehyde in acetic acid gives m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo- quinazolinyl) benzoic acid hydrazones 5. Compounds 5 undergo cyclization with phenoxy acetic acid in the presence of thionyl chloride in dry benzene to furnish 1-[m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo-quinazolinyl- benzamido)]-3-phenoxy-4-phenyl-2-azetidinones 6. The antiviral and antifungal activities of 6 have been reported.
Synthesis and biological activity of isoquinolinyl benzimidazoles
Pandey,Shukla, Aparna
, p. 1381 - 1383 (2007/10/03)
Condensation of benzoic acid with amidoalcohols in presence of conc. H2SO4 furnishes m-(amidoalkyl)-benzoic acids 1 which on treatment with benzoin in polyphosphoric acid give 3,4-diphenyl-7-amidoalkyl-coumarins 2 in excellent yields
