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Volume 26
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Communication

Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides

by
Prakash Chaudhari
1,
Ashley Bunnell
1,
Manivannan Yegambaram
1,
Colette Dooley
2 and
Adel Nefzi
1,3,*
1
Department of Cellular Biology & Pharmacology, Herbert Wertheim College of Medicine, Florida International University, Center for Translational Science, Port Saint Lucie, FL 34987, USA
2
Independent Researcher, Vero Beach, FL 32960, USA
3
Department of Chemistry and Biochemistry, School of Integrated Science and Humanity, College of Arts, Sciences & Education, Florida International University, 11200 S.W. 8th Street, Miami, FL 33199, USA
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2025, 26(17), 8249; https://doi.org/10.3390/ijms26178249 (registering DOI)
Submission received: 10 July 2025 / Revised: 7 August 2025 / Accepted: 20 August 2025 / Published: 25 August 2025
(This article belongs to the Special Issue Drugs—from Chemical Structure to Biological Activity)
Versions Notes

Abstract

Diaza-peptidomimetics are constrained compounds that mimic the biological efficacy of peptides while offering increased stability. We have previously reported the synthesis of bis-cyclic guanidine heterocyclic peptidomimetics as opioid ligands with mixed μ-, κ- and δ-opioid receptor interactions and their potential activity as novel analgesics. Using the same approach, we report here the synthesis of sulfonated and piperazine-tethered bis-cyclic guanidines and their in vitro screening results from radioligand competition binding assays at the μ- (MOR), δ- (DOR), and κ- (KOR) opioid receptors.
Keywords: peptidomimetics; fused heterocyclic compounds; multifunctional; opioid; peripheral-restriction; analgesia; drug discovery; solid-phase synthesis peptidomimetics; fused heterocyclic compounds; multifunctional; opioid; peripheral-restriction; analgesia; drug discovery; solid-phase synthesis

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MDPI and ACS Style

Chaudhari, P.; Bunnell, A.; Yegambaram, M.; Dooley, C.; Nefzi, A. Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides. Int. J. Mol. Sci. 2025, 26, 8249. https://doi.org/10.3390/ijms26178249

AMA Style

Chaudhari P, Bunnell A, Yegambaram M, Dooley C, Nefzi A. Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides. International Journal of Molecular Sciences. 2025; 26(17):8249. https://doi.org/10.3390/ijms26178249

Chicago/Turabian Style

Chaudhari, Prakash, Ashley Bunnell, Manivannan Yegambaram, Colette Dooley, and Adel Nefzi. 2025. "Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides" International Journal of Molecular Sciences 26, no. 17: 8249. https://doi.org/10.3390/ijms26178249

APA Style

Chaudhari, P., Bunnell, A., Yegambaram, M., Dooley, C., & Nefzi, A. (2025). Opioid Affinity of Diazacyclic Peptidomimetic Compounds Derived from Reduced Polyamides. International Journal of Molecular Sciences, 26(17), 8249. https://doi.org/10.3390/ijms26178249

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