What question did this study set out to answer?

Design and synthesize novel unnatural amino acid analogues to incorporate into luteinizing hormone-releasing hormone (LH-RH) antagonists for enhanced potency and prolonged duration.

January 1, 1988Journal of Medicinal Chemistry

Potent, long-acting luteinizing hormone releasing hormone antagonists containing new synthetic amino acids: N,N'-dialkyl-D-homoarginines

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Authors

JNJohn J. NestorAltimmune (United States)RTR. TahilramaniDr. Babasaheb Ambedkar Technological University THTeresa L. HoAgency for Science, Technology and Research

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Implication

Preclinical evaluation reveals potent and prolonged antiovulatory activity in rats, highlighting the therapeutic potential of novel LH-RH antagonists.

Key Points

Design and synthesize novel unnatural amino acid analogues to incorporate into luteinizing hormone-releasing hormone (LH-RH) antagonists for enhanced potency and prolonged duration.
Semisynthesized a series of NG,NG'-dialkyl-D-homoarginine analogues from D-lysine using dialkylcarbodiimides.
Incorporated the unnatural amino acid analogues into LH-RH peptide antagonist sequences.
Evaluated antiovulatory potency and duration of action in a rat antiovulatory assay administered at proestrus or 24 hours earlier at diestrus II.
Incorporation of dialkyl-D-homoarginine analogues conferred high antagonistic potency and extended duration of action.
The lead analogue detirelix demonstrated an ED50 of 0.7 micrograms when administered at noon on proestrus and 2.5 micrograms when administered 24 hours prior at noon on diestrus II in the rat antiovulatory assay.

Cite This Study

Nestor et al. (1988) studied this question.

synapsesocial.com/papers/6a1931fbb71d9c859388beb0 https://doi.org/10.1021/jm00396a011

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Implication

Preclinical evaluation reveals potent and prolonged antiovulatory activity in rats, highlighting the therapeutic potential of novel LH-RH antagonists.

Potent, long-acting luteinizing hormone releasing hormone antagonists containing new synthetic amino acids: N,N'-dialkyl-D-homoarginines

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Cite This Study

Potent, long-acting luteinizing hormone releasing hormone antagonists containing new synthetic amino acids: N,N'-dialkyl-D-homoarginines

Discussion

Member takes

Implication

Key Points

Cite This Study

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