Comparative evaluation of <sup>99m</sup>Tc-MBIP-X/<sup>11</sup>[C] MBMP for visualization of 18 kDa translocator protein

Srivastava, Pooja; Kumari, Neelam; Kakkar, Dipti; Kaul, Ankur; Kumar, Praveer; Tiwari, Anjani K.

doi:10.1039/c9nj00180h

Cited by 8 publications

(6 citation statements)

References 29 publications

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“…The in vivo and ex vivo biodistribution analysis on chloro derivative of MBIP showed a seven-fold higher uptake in heart and 2.5-fold enhanced uptake by heart, and 2.5-fold increased uptake by the lungs as compared to the bromo derivative. [87] Fujinaga et al reported the synthesis of 18 F-labeled radiotracers 104-109 (Figure 25) with improved brain kinetics for PET imaging of TSPO in the glioma and ischemic brain. Bromobenzoxazolone acetic acid 102 (Figure 25) was reacted with 2-methylaminopyridine, N-methylaniline, and 4-methylaminopyridine in the presence of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (WSC) and hydroxybenzotriazole (HOBt) to procure the final acetamidobenzoxazolones.…”

Section: Translocator Protein (Tspo) Inhibitorsmentioning

confidence: 99%

Synthesis and biological profile of benzoxazolone derivatives

Prasher

Mall

Sharma

2023

Archiv der Pharmazie

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The benzoxazolone nucleus is an ideal scaffold for drug design, owing to its discrete physicochemical profile, bioisosteric preference over pharmacokinetically weaker moieties, weakly acidic behavior, presence of both lipophilic and hydrophilic fragments on a single framework, and a wider choice of chemical modification on the benzene and oxazolone rings. These properties apparently influence the interactions of benzoxazolone‐based derivatives with their respective biological targets. Hence, the benzoxazolone ring is implicated in the synthesis and development of pharmaceuticals with a diverse biological profile ranging from anticancer, analgesics, insecticides, anti‐inflammatory, and neuroprotective agents. This has further led to the commercialization of several benzoxazolone‐based molecules and a few others under clinical trials. Nevertheless, the SAR exploration of benzoxazolone derivatives for the identification of potential “hits” followed by the screening of “leads” provides a plethora of opportunities for further exploration of the pharmacological profile of the benzoxazolone nucleus. In this review, we aim to present the biological profile of different derivatives based on the benzoxazolone framework.

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Section: Translocator Protein (Tspo) Inhibitorsmentioning

confidence: 99%

Synthesis and biological profile of benzoxazolone derivatives

Prasher

Mall

Sharma

2023

Archiv der Pharmazie

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“…Conventionally, the earliest TSPO ligand was benzodiazepine [ 11 C]-Ro5–4864 that differentiated peripheral and central benzodiazepine receptors . Diverse TSPO ligands from various structural classes such as isoquinoline carboxamides (e.g., [ 11 C]-PK-11195, [ 11 C]-ER176), benzodiazepines (e.g., [ 11 C]-Ro5–4864), phenoxyarylacetamides (e.g., [ 11 C]-DAA1106), aryloxyanilides (e.g., [ 11 C]-PBR28), 2-phenyl-imidazo[1,2- a ]pyridine acetamides (e.g., alpidem), and pyrazolopyrimidines ([ 18 F]-DPA-714) have been described. − Figure encloses famously used first-, second-, and third-generation ligands. Besides different endogenous biomolecules such as cholesterol or compound porphyrin, TSPO exhibits binding to a range of synthetic ligands.…”

Section: Tspo Pet Tracers-current Statusmentioning

confidence: 99%

Mapping of Translocator Protein (18 kDa) in Peripheral Sterile Inflammatory Disease and Cancer through PET Imaging

Adhikari

Singh

Mahar³

et al. 2021

Mol. Pharmaceutics

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Positron emission tomography (PET) imaging of the translocator 18 kDa protein (TSPO) with radioligands has become an effective means of research in peripheral inflammatory conditions that occur in many diseases and cancers. The peripheral sterile inflammatory diseases (PSIDs) are associated with a diverse group of disorders that comprises numerous enduring insults including the cardiovascular, respiratory, gastrointestinal, or musculoskeletal system. TSPO has recently been introduced as a potential biomarker for peripheral sterile inflammatory diseases (PSIDs). The major critical issue related to PSIDs is its timely characterization and localization of inflammatory foci for proper therapy of patients. As an alternative to metabolic imaging, protein imaging expressed on immune cells after activation is of great importance. The five transmembrane domain translocator protein-18 kDa (TSPO) is upregulated on the mitochondrial cell surface of macrophages during inflammation, serving as a potential ligand for PET tracers. Additionally, the overexpressed TSPO protein has been positively correlated with various tumor malignancies. In view of the association of escalated TSPO expression in both disease conditions, it is an immensely important biomarker for PET imaging in oncology and PSIDs. In this review, we summarize the most outstanding advances on TSPO-targeted PSIDs and cancer in the development of TSPO ligands as a potential diagnostic tool, specifically discussing the last five years.

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“…The visualization of overexpressed microglial cells in the living brain by high affinity and selective PET tracers has been considered as a powerful tool for staging the neuroinflammation. 22 , 23 The development of PET tracers was initially started in the mid-1980s using positron emitter isotopes 11 C and 18 F. 24 PET tracers have much potential for in vivo molecular imaging and play a most impressive role for the assessment and staging of neuroinflammation. 25 PET tracers of TSPO have been categorized in three generations, which are presented in Figure 3 .…”

Section: Introductionmentioning

confidence: 99%

The 18-kDa Translocator Protein PET Tracers as a Diagnostic Marker for Neuroinflammation: Development and Current Standing

et al. 2022

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Translocator protein (TSPO, 18 kDa) is an evolutionary, well-preserved, and tryptophan-rich 169-amino-acid protein which localizes on the contact sites between the outer and inner mitochondrial membranes of steroid-synthesizing cells. This mitochondrial protein is implicated in an extensive range of cellular activities, including steroid synthesis, cholesterol transport, apoptosis, mitochondrial respiration, and cell proliferation. The upregulation of TSPO is well documented in diverse disease conditions including neuroinflammation, cancer, brain injury, and inflammation in peripheral organs. On the basis of these outcomes, TSPO has been assumed to be a fascinating subcellular target for early stage imaging of the diseased state and for therapeutic purposes. The main outline of this Review is to give an update on dealing with the advances made in TSPO PET tracers for neuroinflammation, synchronously emphasizing the approaches applied for the design and advancement of new tracers with reference to their structure–activity relationship (SAR).

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Comparative evaluation of ^99mTc-MBIP-X/¹¹[C] MBMP for visualization of 18 kDa translocator protein

Abstract: An elevated translocator protein (18 kDa, TSPO) density is observed during inflammation in the brain and peripheral organs making it a viable target for imaging.

Cited by 8 publications

References 29 publications

Synthesis and biological profile of benzoxazolone derivatives

Synthesis and biological profile of benzoxazolone derivatives

Mapping of Translocator Protein (18 kDa) in Peripheral Sterile Inflammatory Disease and Cancer through PET Imaging

The 18-kDa Translocator Protein PET Tracers as a Diagnostic Marker for Neuroinflammation: Development and Current Standing

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Comparative evaluation of 99mTc-MBIP-X/11[C] MBMP for visualization of 18 kDa translocator protein

Abstract: An elevated translocator protein (18 kDa, TSPO) density is observed during inflammation in the brain and peripheral organs making it a viable target for imaging.

Cited by 8 publications

References 29 publications

Synthesis and biological profile of benzoxazolone derivatives

Synthesis and biological profile of benzoxazolone derivatives

Mapping of Translocator Protein (18 kDa) in Peripheral Sterile Inflammatory Disease and Cancer through PET Imaging

The 18-kDa Translocator Protein PET Tracers as a Diagnostic Marker for Neuroinflammation: Development and Current Standing

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Comparative evaluation of ^99mTc-MBIP-X/¹¹[C] MBMP for visualization of 18 kDa translocator protein