218608-82-3Relevant articles and documents
Protein-protein interface mimicry by an oxazoline piperidine-2,4-dione
Li, Xun,Taechalertpaisarn, Jaru,Xin, Dongyue,Burgess, Kevin
supporting information, p. 632 - 635 (2015/03/05)
Representative minimalist mimics 1 were prepared from amino acids. Scaffold 1 was not designed to mimic any particular secondary structure, but simulated accessible conformations of this material were compared with common ideal secondary structures and with >125000 different protein-protein interaction (PPI) interfaces. This data mining exercise indicates that scaffolds 1 can mimic features of sheet-turn-sheets, somewhat fewer helical motifs, and numerous PPI interface regions that do not resemble any particular secondary structure.
Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain
Sinha, Manish,Dola, Vasanth R.,Agarwal, Pooja,Srivastava, Kumkum,Haq, Wahajul,Puri, Sunil K.,Katti, Seturam B.
, p. 3573 - 3586 (2014/07/07)
Emergence and spread of multidrug resistant strains of Plasmodium falciparum has severely limited the antimalarial chemotherapeutic options. In order to overcome the obstacle, a set of new side-chain modified 4-aminoquinolines were synthesized and screened against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of P. falciparum. The key feature of the designed molecules is the use of methylpiperazine linked α, β3- and γ-amino acids to generate novel side chain modified 4-aminoquinoline analogues. Among the evaluated compounds, 20c and 30 were found more potent than CQ against K1 and displayed a four-fold and a three-fold higher activity respectively, with a good selectivity index (SI = 5846 and 11,350). All synthesized compounds had resistance index between 1.06 and >14.13 as against 47.2 for chloroquine. Biophysical studies suggested that this series of compounds act on heme polymerization target.
Wolff rearrangement of Nα-Boc-/Z-protected aminodiazoketones to the corresponding β-amino acids under microwave irradiation
Kantharaju,Patil, Basanagoud S.,Suresh Babu, Vommina V.
, p. 2611 - 2613 (2007/10/03)
The Wolff rearrangement of Nα-Boc-/Z-protected aminodiazoketones in the presence of silver benzoate under microwave irradiation is described. The reaction is found to be rapid, efficient and complete. It results in the isolation of Boc-/Z- prot
Homologation of α-amino acids to β-amino acids: 9-Fluorenylmethyl chloroformate as a carboxyl group activating agent for the synthesis of Nα-protected aminoacyldiazomethanes
Kantharaju,Suresh Babu, Vommina V.
, p. 2152 - 2158 (2007/10/03)
An efficient and stereospecific homologation of urethane-protected α-amino acids to β-amino acids by Arndt-Eistert approach using an equimolar mixture of Fmoc-/Boc-/Z-α-amino acid and 9-fluorenylmethyl chloroformate for the acylation of diazomethane synth
Homologation of α-amino acids to β-amino acids using Boc2O
Vasanthakumar, Ganga-Ramu,Patil, Basanagoud S.,Suresh Babu, Vommina V.
, p. 2087 - 2089 (2007/10/03)
The use of Boc2O as a coupling agent in the homologation of N-urethane protected-α-amino acid to its β-homomers by the Arndt-Eistert method is described. The homologation gives good yields without racemization. The use of Boc2O as a
Synthesis of angiotensin II analogues by incorporating beta-homotyrosine or beta-homoisoleucine residues.
Stachowiak,K. et al.
, p. 1128 - 1130 (2007/10/07)
[1-Sarcosine,4-beta-homotyrosine]-(I), [5-beta-homoisoleucine]-(II), and [1-sarcosine,5-beta-homoisoleucine]angiotensin II (III) were synthesized by Merrifield''s solid-phase procedure to study the effect of pressor activity and duration of action. The an
