21855-73-2Relevant articles and documents
C-4 " substituted Macrolides compd.
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Paragraph 0026; 0027, (2016/10/08)
A useful novel compound that shows superior antibacterial activity also against erythromycin resistant bacteria, for example, resistant pneumococci, streptococci, mycoplasmas, and the like, against which sufficient antibacterial activity cannot be obtaine
Application of Predictive QSAR Models to Database Mining: Identification and Experimental Validation of Novel Anticonvulsant Compounds
Shen, Min,Béguin, Cécile,Golbraikh, Alexander,Stables, James P.,Kohn, Harold,Tropsha, Alexander
, p. 2356 - 2364 (2007/10/03)
We have developed a drug discovery strategy that employs variable selection quantitative structure-activity relationship (QSAR) models for chemical database mining. The approach starts with the development of rigorously validated QSAR models obtained with
2-Alkynyl-8-aryladenines possessing an amide moiety: Their synthesis and structure-activity relationships of effects on hepatic glucose production induced via agonism of the A2B adenosine receptor
Harada,Asano,Kawata,Inoue,Horizoe,Yasuda,Nagata,Murakami,Nagaoka,Kobayashi,Tanaka,Abe
, p. 2709 - 2726 (2007/10/03)
A series of 2-alkynyl-8-aryladenine derivatives bearing an amide moiety at the 9-position of adenine was synthesized. These analogues were evaluated for inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes. The m-primary benzamide derivative 15f was the most potent compound (IC50 = 0.017 μM), being 15-fold more active than the corresponding 9-methyl derivative (1). Compound 15f showed 72- and 5.2-fold selectivity for human A2B receptor versus human A1 and A2A receptors, respectively. Structure-activity relationship (SAR) studies of the synthesized compounds indicated that a three-carbon linker, fixed in the form of a benzene ring, between the adenine core and the amide moiety is important for both A2B antagonistic activity and selectivity. The IC50 values in rat hepatocyte glucose assay correlated well with the IC50 values in cAMP assay using Chinese hamster ovary cells stably transfected with human A2B receptors (r2 = 0.94). The A1 and A2A affinities showed no correlation with the potency to inhibit NECA-induced glucose production. These results strongly support our previous conclusion that adenosine agonist-induced hepatic glucose production in rat hepatocytes is mediated through the A2B receptor.
Peptide Synthesis with Benzo- and Naphthosultones
Acher, Francine,Wakselman, Michel
, p. 4133 - 4138 (2007/10/02)
6-Nitro- and 6,8-dinitronaphth-1,2-oxathiole S,S-dioxides (7b and 7c) have been prepared from the parent naphthosultone 7a and compared with 5-nitrobenz-3H-1,2-oxathiole S,S-dioxide (1b) as coupling reagents for peptide synthesis.Nucleophilic attack of a carboxylate salt on these strained five-membered sultones leads to activated esters 3 and 9 which rapidly react with amines (except in the case of 9c).The rate constant for the formation of ester 9b is higher than that of 3b.Amides or peptides are formed in slightly better yields with the naphthosultone 7b than with the benzosultone 1b.The naphthosultones are also preferred over the benzosultones from the point of view of amount of 5(4H)-oxazolone formation from N-benzoyl amino acids and the degree of racemization.However the rate of alkaline hydrolysis of 7b is slower than that of 1b.All these results may be rationalized by a better intramolecular acyl transfer reaction in the more rigid mixed anhydride intermediate 8b.There is no dependence on in the rate equation for aminolysis of esters 3b and 9b by benzylamine in THF, acetonitrile, or DMF and the aminolysis is probably anchimerically assisted by a neighbouring S=O group.Esters 3b are more selective acylating agents for primary amino groups in the presence of secondary ones than esters 9b and this observation is exploited in a synthesis of maytenine by selective acylation of spermidine.
Transition Metal Ions and Amides. VIII. Discrimination between Different Models for the Complexation of Cu2+ with N,N'-Diglycyl-1,2-ethanediamine, N,N'-Diglycyl-1,3-propanediamine and Glycine Ethylamide by Potentiometric or by Spectrophotometri
Briellmann, Markus,Zuberbuehler, Andreas D.
, p. 46 - 54 (2007/10/02)
The complexation of Cu2+ with 1,8-diamino-3,6-diaza-2,7-octanedione (=N,N'-diglycyl-1,2-ethanediamine, DED) and with 1,9-diamino-3,7-diaza-2,8-nonanedione (=N,N'-diglycyl-1,3-propanediamine, DPD) has been studied by potentiometric and by spectr
