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1982 (1)
1Author    Karl Folkers, CyrilY. Bowers+, WilsonB. Lutz, Klaus Friebel, Teresa Kubiak, Bernhard Schircks, Georg RampoldRequires cookie*
 Title    Synthesis and Bioassay of Antagonists of the Luteinizing Hormone Releasing Hormone Having the Azagly 10 Moiety  
 Abstract    Seven new analogs of the luteinizing hormone releasing hormone (LHRH), having an Azagly 10 moiety, and three corresponding Gly 10 -analogs were synthesized for bioassay and comparison of inhibitory potencies. This study was toward a possible advantage of the Azagly 10 moiety to minimize C-terminal degradation, in vivo. Of the three procedures which were studied to achieve Azagly 10 -peptides, the reaction of cyanate ion with hydrazides was the most favorable. Variations of substitution in position 1 were also studied. The data from the antiovulatory assay showed that an Azagly 10 moiety may not depress activity, and may allow equal or even higher activity than the Glv 10 moiety, depending on the analog. [N-Ac-D-Thr 1 , D-p-Cl-Phe 2 , D-Trp 3 -6 , Azagly 10 ] LHRH was more inhibitory than the corresponding Gly 10 -analog. Based on pairs of analogs, the following relationships appeared: (1) N-Ac-D-Thr 1 was more effective than N-Ac-jo-Cl-Phe 1 ; (2) The L-configuration of Ala as N-Ac-Ala 1 -was more effective than the D—; (3) N-Ac-Ala 1 appeared more effective than the N-Ac-D-Thr 1 ; (4) D-Trp 6 appeared more effective than D-Phe 6 . In an ultimate clinical use of an antagonist of LHRH to block ovulation, the Azagly 10 moiety may be advantageous for limitation of enzymatic degradation. 
  Reference    Z. Naturforsch. 37b, 1075—1081 (1982); received March 23 1982 
  Published    1982 
  Keywords    Antagonist, Luteinizing Hormone Releasing Hormone, Ovulation, Peptides, Azaglycine 
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 TEI-XML for    default:Reihe_B/37/ZNB-1982-37b-1075.pdf 
 Identifier    ZNB-1982-37b-1075 
 Volume    37