| 1 | Author
| Karl Folkers, CyrilY. Bowers, Teresa Kubiak, Janusz Stepinski | Requires cookie* | | Title
| Synthesis and Antiovulatory Activities in Rats of Analogs of the Luteinizing Hormone Releasing Hormone Having a Moiety of /?-(3-Quinolyl)-D-a-alanine in Positions 3 and 6  | | | Abstract
| Analogs of the luteinizing hormone releasing hormone (LHRH) having a moiety (D-Qal-) of/3-(3-quinolyl)-D-a-alanine were synthesized toward more effective inhibitors of ovulation. [N-Ac-^Cl-D-Phe 1 -2 , D-3-Pal 3 , D-3-Qal 6 , D-Ala 10 ]-LHRH was the most effective, and had an antiovulatory activity of 40% at 1 /ig/rat. D-3-Qal 6 was as effective as D-Trp 6 in combination with N-Ac-3 z1 Pro 1 , ^oF-D-Phe 2 , D-Trp 3 . D-Arg 6 was superior to D-3-Qal 6) in combination with N-Ac-^Cl-D-Phe 1 ' 2 , D-Trp 3 (or D-3-Pal 3), D-Ala 10 . The introduction of D-3-Qal 3 , D-His 3 and D-Arg 3 in comparable analogs caused sub-stantial loss of activities. Abbreviations D-3-Pal = /S-(3-pyridyl)-D-a-alanine; D-3-Qal = ß-(3-quinolyl)-D-a-alanine; BOC = fertf-butyloxy-carbonyl; ÄOC = tferf-amyloxycarbonyl; DCC = N,N'-dicyclohexylcarbodiimide; 3 ZlPro = 3,4-dehydro-L-proline; pF-D-Phe — yara-fluoro-D-phenylalanine; ^Cl-D-Phe = ^»am-ehloro-D-phenylalanine; Ac = acetyl, HPLC = high performance liquid chromato-graphy. | | |
Reference
| Z. Naturforsch. 38b, 1253—1256 (1983); received June 27 1983 | | |
Published
| 1983 | | |
Keywords
| Ovulation, Hormone, Antagonist, Quinolylalanine, Luteinizing Hormone Releasing Hormone | | |
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| default:Reihe_B/38/ZNB-1983-38b-1253.pdf | | | Identifier
| ZNB-1983-38b-1253 | | | Volume
| 38 | |
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