Loading...
  • cyclic
  • To confront the limitations associated with cyclic tetrapeptides as β-turn mimics, we have designed and structurally analyzed 2 alternative classes of 13- or 14-membered ring pseudotetrapeptides containing either 1 or 2 triazole moieties, respectively (Fig. 1). (scripps.edu)
  • Chemical and molecular structures of representative members of 2 classes of cyclic pseudotetrapeptide scaffolds. (scripps.edu)
  • Using the rigid scaffold strategy described earlier, we have gathered evidence that the more potent conformation of apicidin, an archetypal member of a family of naturally occurring cyclic tetrapeptide inhibitors of histone deacetylases (HDACs), is not the previously believed all- trans ( t-t-t-t ) structure that predominates in solution, but rather a cis-trans-trans-trans ( c-t-t-t ) conformation (Fig. 2). (scripps.edu)
  • Our approach relies on the design, synthesis, structural characterization, and functional analysis of a series of cyclic pseudotetrapeptides bearing 1,4- or 1,5-disubstituted 1,2,3-triazole amino acids that serve as trans - or cis -amide bond surrogates, respectively. (scripps.edu)
  • denoting a cyclic compound. (thefreedictionary.com)
  • identical
  • The 3-dimensional pharmacophoric display of the pseudotetrapeptides is systematically altered by varying the stereochemistry around the otherwise constitutionally identical scaffolds, yielding both compounds with broad-spectrum activity against the 5 human somatostatin receptor subtypes and compounds with receptor selectivity. (scripps.edu)
  • A substance is composed of identical atoms. (cueflash.com)
  • 2 or more orbitals mix to form identical hybrid orbitals. (cram.com)
  • selectivity
  • Compound 2 was designed from compound 1 by methylating the pyridine giving a highly soluble compound with extended rat lung t½, increased potency, maintained selectivity profile, very low logD and low plasma protein binding (Table1). (nih.gov)
  • receptor
  • Therefore, the C2 side chain in compound 2 underlines dramatic improvement of rat lung retention together with gain of new interactions between A2a receptor and compound 2. (nih.gov)
  • epoxy
  • where the equivalent ratio of the (B)(1) and (B)(2) in the clearcoat film-forming composition is adjusted such that for each equivalent of epoxy, there are around 0.3 to around 3.0 equivalents of carboxyl. (google.com.au)
  • salts
  • 5-Methylthio-2-oxo-2,3-dihydro-1H-imidazo[1,2-c]thiazolium salts readily react with 3-ethylrhodanine, p-dimethylaminobenzaldehyde, and 3-ethyl-2-methylbenzothiazolium tosylate with the formation of polymethine dyes, including dyes with a mesoionic structure. (springer.com)
  • least
  • A two component curable composition is prepared by mixing (I) a main material composition or a solution thereof comprising the compound (A) and the compound (B) or a self-crosslinkable compound (D), and (II) an acid catalyst or the solution comprising at least one of a Bronsted acid, a Lewis acid or a mixture of a metallic chelate compound and a compound having a silanol group. (google.com.au)
  • Structure
  • Figure13 illustrates the binding mode of compound 2 docked into the X-ray A2a crystallographic structure in the agonistic conformation (Lebon et al. (nih.gov)
  • In the process of chelation, picolinic acid ( PA ), known also as 2-pyridine carboxylic acid to biochemists, is able to attract a positively charged ion into its larger molecular structure and shield the charge so that the ion appears to be neutral or negatively charged. (fsu.edu)
  • Chemical
  • Picloram, the organic chemical 4-amino-3,5,6-trichloropyridine-2-carboxylic acid, and known to foresters, range managers, and highway departments as the trade product Tordon, is usually applied to cut tree stumps, as a potassium salt, to prevent resprouting. (fsu.edu)
  • functional
  • Although effective drug scaffolds have been developed to precisely position up to 4 functional groups primarily in 2 dimensions, an analogous rigid scaffold capable of predictably juxtaposing 4 amino acid side chains in 3 dimensions has not been readily available. (scripps.edu)
  • protein
  • Compound 2, in comparison to a reference A2a agonist, UK-432,097, demonstrated higher solubility, lower lipophilicity, lower plasma protein binding, high rat lung retention (28% remaining after 24 h), and was efficacious in a lung inflammatory rat model following intratracheal dosing. (nih.gov)
  • A fundamental strategy in rationally designing synthetic compounds to bind a protein of interest is to use a known ligand as a structural model to specify the precise conformational and pharmacophoric requirements for binding. (scripps.edu)
  • characterization
  • In this paper, we describe the discovery and characterization of a new, potent and selective A2a agonist (compound 2) with prolonged lung retention and limited systemic exposure following local administration. (nih.gov)