Structural modification and biological evaluation of Dmt1-DALDA analogues
نویسندگان
چکیده
منابع مشابه
Dansylated analogues of the opioid peptide [Dmt1]DALDA: in vitro activity profiles and fluorescence parameters.
Dansylated analogues of the potent and selective micro opioid peptide agonist [Dmt(1)]DALDA (H-Dmt-D-Arg-Phe-Lys-NH(2); Dmt = 2',6'-dimethyltyrosine) were prepared either by substitution of N(beta)-dansyl-alpha,beta-diaminopropionic acid or N(epsilon)-dansyllysine for Lys(4), or by attachment of a dansyl group to the C-terminal carboxamide function via a linker. All three analogues displayed hi...
متن کاملDALDA analogues containing -hydroxymethylamino acids
To evaluate the role of aromatic amino-acids residues, four analogues of the -selective opioid peptide agonist DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) containing the amphiphilic, , -disubstituted amino acid (R)or (S)-hydroxymethyltyrosine (HmTyr) in position 1 and (R)or (S)-hydroxymethylphenylalanine (HmPhe) in position 3 of the peptide sequence were synthesized. Only the [(R)-HmPhe 3 )]DALDA analogue ...
متن کاملAntinociceptive and respiratory effects of intrathecal H-Tyr-D-Arg-Phe-Lys-NH2 (DALDA) and [Dmt1] DALDA.
DALDA (H-Tyr-D-Arg-Phe-Lys-NH(2)) and [Dmt(1)]DALDA (H-Dmt-D-Arg-Phe-Lys-NH(2)) (Dmt = 2',6'-dimethyltyrosine) are potent and highly selective mu-opioid agonists (K(i)(delta)/K(i)(mu) > 10,000 and K(i)(kappa)/K(i)(mu) > 100). Both peptides carry a 3+ charge at physiological pH. Their antinociceptive and respiratory effects were compared with morphine (MOR) after intrathecal administration in ra...
متن کاملOxyresveratrol: Structural Modification and Evaluation of Biological Activities.
Oxyresveratrol (2,4,3',5'-tetrahydroxystilbene, 1), a phytoalexin present in large amounts in the heartwood of Artocarpus lacucha Buch.-Ham., has been reported to possess a wide variety of biological activities. As part of our continuing studies on the structural modification of oxyresveratrol, a library of twenty-six compounds was prepared via O-alkylation, aromatic halogenation, and electroph...
متن کاملNovel Linezolid like Analogues: Synthesis, Characterization and Biological Evaluation
The synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one was achieved in two steps, In first step, pyrazine-2-carboxamide dissolved in EtOH, 10% KOH solution with ClCH2COOH produced compound 2-(pyrazine-2-carboxamido) acetic acid (II) and in second step, compound (II) in (CH3CO)2O with aromatic aldehyde, and catalyst potassium ace...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Pharmacological Reports
سال: 2011
ISSN: 1734-1140
DOI: 10.1016/s1734-1140(11)70451-0