Design, synthesis, inhibition studies, and molecular modeling of pepstatin analogues addressing different secreted aspartic proteinases of Candida albicans

2013 ◽  
Vol 85 (7) ◽  
pp. 881-887 ◽  
Author(s):  
Cosimo D. Cadicamo ◽  
Jérémie Mortier ◽  
Gerhard Wolber ◽  
Marie Hell ◽  
Ina E. Heinrich ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Molecular Modeling ◽  
Aspartic Proteinases ◽  
Design Synthesis ◽  
Synthesis Inhibition ◽  
Inhibition Studies

Peptide Inhibitors of Aspartic Proteinases with Hydroxyethylene Isostere Replacement of Peptide Bond. II. Preparation of Pseudotetrapeptides Derived from Diastereoisomeric 5-Amino-2-benzyl-4-hydroxy-6-phenylhexanoic Acids

1998 ◽  
Vol 63 (4) ◽  
pp. 541-548 ◽  
Author(s):  
Jaroslav Litera ◽  
Jan Weber ◽  
Ivana Křížová ◽  
Iva Pichová ◽  
Jan Konvalinka ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Peptide Bond ◽  
Peptide Inhibitors ◽  
Aspartic Proteinases ◽  
Hiv 1

Twelve pseudotetrapeptides, Boc-NHCH(CH2Ph)CH(OH)CH2CH(CH2Ph) CO-Xaa-Phe-NH2 9-11, were prepared by [(benzotriazol-1-yl)oxy]tris(dimethylamino)phosphonium hexafluorophosphate-mediated couplings of diastereoisomeric O-silylated (2R or 2S,4R or 4S,5S)-2-benzyl-5-(tert-butoxycarbonyl)amino-4-hydroxy-6-phenylhexanoic acids 1 with dipeptides H-Xaa-Phe-NH2 (Xaa = Gln, Glu(OBzl) or Ile) 3-5, followed by O-deprotection. Pseudotetrapeptides 9-11 were tested for inhibition of aspartic proteinases secreted by Candida albicans and C. tropicalis. The level of inhibition of both yeast proteinases was very low, contrasting with the nanomolar IC50 values obtained for inhibition of HIV-1 proteinase.

Design, synthesis and molecular modeling of new quinazolin-4(3H)-one based VEGFR-2 kinase inhibitors for potential anticancer evaluation

2021 ◽  
Vol 109 ◽  
pp. 104695
Author(s):  
Abdallah E. Abdallah ◽  
Sally I. Eissa ◽  
Maged Mohammed Saleh Al Ward ◽  
Reda R. Mabrouk ◽  
Ahmed B.M. Mehany ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Kinase Inhibitors ◽  
Design Synthesis

scholarly journals Design, synthesis, antimicrobial activity and molecular modeling studies of novel benzofuroxan derivatives against Staphylococcus aureus

2009 ◽  
Vol 17 (8) ◽  
pp. 3028-3036 ◽  
Author(s):  
Salomão Dória Jorge ◽  
Andrea Masunari ◽  
Carlota Oliveira Rangel-Yagui ◽  
Kerly Fernanda Mesquita Pasqualoto ◽  
Leoberto Costa Tavares
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Molecular Modeling ◽  
Design Synthesis ◽  
Modeling Studies ◽  
Molecular Modeling Studies

Two novel series of allocolchicinoids with modified seven membered B-rings: design, synthesis, inhibition of tubulin assembly and cytotoxicity

2005 ◽  
Vol 13 (10) ◽  
pp. 3497-3511 ◽  
Author(s):  
Frank Büttner ◽  
Silke Bergemann ◽  
Daniel Guénard ◽  
Ronald Gust ◽  
Gunther Seitz ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Synthesis Inhibition
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