Quest for novel chemical entities through incorporation of silicon in drug scaffolds

R Ramesh, DS Reddy - Journal of Medicinal Chemistry, 2017 - ACS Publications
In order to optimize a lead molecule for further development, bioisosteric replacements are
generally adopted as one of the strategies. Silicon appears to be the right choice as a …

Silicon-containing amino acids: synthetic aspects, conformational studies, and applications to bioactive peptides

E Rémond, C Martin, J Martinez, F Cavelier - Chemical Reviews, 2016 - ACS Publications
Unnatural α-amino acids form a family of essential molecules used for, among other
applications, the synthesis of modified peptides, to improve resistance to proteolytic enzyme …

Novel approaches, drug candidates, and targets in pain drug discovery

S Obeng, T Hiranita, F León, LR McMahon… - Journal of medicinal …, 2021 - ACS Publications
Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …

Unnatural amino acids: Promising implications for the development of new antimicrobial peptides

X Wang, X Yang, Q Wang, D Meng - Critical Reviews in …, 2023 - Taylor & Francis
The increasing incidence and rapid spread of bacterial resistance to conventional antibiotics
are a serious global threat to public health, highlighting the need to develop new …

New insights in the design of bioactive peptides and chelating agents for imaging and therapy in oncology

AL Tornesello, L Buonaguro, ML Tornesello… - Molecules, 2017 - mdpi.com
Many synthetic peptides have been developed for diagnosis and therapy of human cancers
based on their ability to target specific receptors on cancer cell surface or to penetrate the …

Therapeutic approaches targeting the neurotensin receptors

MR Iyer, G Kunos - Expert Opinion on Therapeutic Patents, 2021 - Taylor & Francis
Introduction: Neurotensin is a gut-brain peptide hormone, a 13 amino acid neuropeptide
found in the central nervous system and in the GI tract. The neurotensinergic system is …

Neurotensin (8–13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease

T Kühl, MG Georgieva, H Hübner, M Lazarova… - European Journal of …, 2023 - Elsevier
The modulatory interactions between neurotensin (NT) and the dopaminergic
neurotransmitter system in the brain suggest that NT may be associated with the progression …

Structural optimization and characterization of potent analgesic macrocyclic analogues of neurotensin (8–13)

M Sousbie, M Vivancos, RL Brouillette… - Journal of Medicinal …, 2018 - ACS Publications
The neurotensin receptors are attractive targets for the development of new analgesic
compounds. They represent potential alternatives or adjuvants to opioids. Herein, we report …

Recent progress in non-opioid analgesic peptides

MJP de Vega, A Ferrer-Montiel… - Archives of biochemistry …, 2018 - Elsevier
Pain is a prevalent complex medical problem, characterized by physically debilitating and
mentally destabilizing conditions. Current pain therapeutics mainly include non-steroidal …

MnO2 mediated sequential oxidation/olefination of alkyl-substituted heteroarenes with alcohols

C Zhang, Z Li, Y Fang, S Jiang, M Wang, G Zhang - Tetrahedron, 2020 - Elsevier
A practical and efficient ligand-free MnO 2 mediated sequential oxidation and olefination
has been developed for the facile synthesis of a broad range of unsaturated N …