Susovan Jana

National Institute of Mental Health

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Co-Authors

Victor W. Pike

National Institute of Mental Health

Sanjay Telu

National Institute of Mental Health

Jimmy E. Jakobsson

National Institute of Mental Health

Sami S. Zoghbi

National Institutes of Health

Cheryl L. Morse

National Institute of Mental Health

Qunchao Zhao

National Institute of Mental Health

Robert B. Innis

National Institute of Mental Health

Bo Yeun Yang

National Institutes of Health

Salvatore D. Lepore

Florida Atlantic University

Shawn Wu

National Institute of Mental Health

Cooperative Institutions

National Institutes of Health

National Institute of Mental Health

National Institute on Alcohol Abuse and Alcoholism

National Institute of Mental Health

Karolinska Institutet

National Cancer Institute

University of Chicago

National Institute on Drug Abuse

Case Western Reserve University

Center for Cancer Research

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Papers

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Development of a Candidate PET Radioligand for Receptor Interacting Protein 1 Kinase (RIPK1) and Evaluation in Healthy Monkey

Nuclear Medicine and Biology (2023)

Susovan Jana Sanjay Telu Aneesh Tazhe Veetil Jimmy E. Jakobsson Sami S. Zoghbi

Radioligand

Radioligand Assay

10.1016/j.nucmedbio.2023.108580

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Citations (0)

Crown Ether Nucleophilic Catalysts (CENCs): Agents for Enhanced Silicon Radiofluorination

The Journal of Organic Chemistry (2017)

Susovan Jana Mohammed H. Al‐Huniti Bo Yang Shuiyu Lu Victor W. Pike

New bifunctional phase transfer agents were synthesized and investigated for their abilities to promote rapid fluorination at silicon. These agents, dubbed crown ether nucleophilic catalysts (CENCs), are 18-crown-6 derivatives containing a side-arm and a potentially nucleophilic hydroxyl group. These CENCs proved efficacious in the fluorination of hindered silicon substrates, with fluorination yields dependent on the length of linker connecting the metal chelating unit to the hydroxyl group. The efficacy of these CENCs was also demonstrated for rapid radiofluorination under mild conditions for eventual application in molecular imaging with positron emission tomography (PET). The hydrolysis-resistant aryl silicon fragment is promising as a convenient synthon for labeling potential PET radiotracers.

Synthon

Linker

18-Crown-6

Williamson ether synthesis

10.1021/acs.joc.6b02457

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Citations (8)

Synthesis of Novel C-Pivot Lariat 18-Crown-6 Ethers and Their Efficient Purification

Synlett (2015)

Salvatore D. Lepore Susovan Jana Vallabh Suresh

The syntheses of various lariat ethers including several not previously reported and their efficient purification are presented. The synthesis route brings together reactions from a variety of previous works leading to a robust and generalized approach to these C-pivot lariats. The main steps are condensation of functionalized diols with pentaethylene glycol ditosylate in the presence of potassium as a templating cation. Purification of the final products was achieved without chromatography by extracting from an aqueous potassium hydroxide solution.

Potassium hydroxide

10.1055/s-0034-1378790

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Citations (3)

Rapid and Efficient Syntheses of [11C]Trifluoroethoxy Heteroarenes with a Novel 11C-Labeling Synthon, [11C]CF3CH2OK

Nuclear Medicine and Biology (2023)

Qunchao Zhao Sanjay Telu Susovan Jana Victor W. Pike

Synthon

10.1016/j.nucmedbio.2023.108429

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Broad Scope and High‐Yield Access to Unsymmetrical Acyclic [¹¹C]Ureas for Biomedical Imaging from [¹¹C]Carbonyl Difluoride

Chemistry - A European Journal (2021)

Jimmy E. Jakobsson Sanjay Telu Shuiyu Lu Susovan Jana Victor W. Pike

Abstract Effective methods are needed for labelling acyclic ureas with carbon‐11 ( t 1/2 =20.4 min) as potential radiotracers for biomedical imaging with positron emission tomography (PET). Herein, we describe the rapid and high‐yield syntheses of unsymmetrical acyclic [ 11 C]ureas under mild conditions (room temperature and within 7 min) using no‐carrier‐added [ 11 C]carbonyl difluoride with aliphatic and aryl amines. This methodology is compatible with diverse functionality (e. g., hydroxy, carboxyl, amino, amido, or pyridyl) in the substrate amines. The labelling process proceeds through putative [ 11 C]carbamoyl fluorides and for primary amines through isolable [ 11 C]isocyanate intermediates. Unsymmetrical [ 11 C]ureas are produced with negligible amounts of unwanted symmetrical [ 11 C]urea byproducts. Moreover, the overall labelling method tolerates trace water and the generally moderate to excellent yields show good reproducibility. [ 11 C]Carbonyl difluoride shows exceptional promise for application to the synthesis of acyclic [ 11 C]ureas as new radiotracers for biomedical imaging with PET.

Isocyanate

Radiosynthesis

10.1002/chem.202100690

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Citations (6)

Isotopologues of potassium 2,2,2-trifluoroethoxide for applications in positron emission tomography and beyond

Nature Communications (2024)

Qunchao Zhao Sanjay Telu Susovan Jana Cheryl L. Morse Victor W. Pike

Abstract The 2,2,2-trifluoroethoxy group increasingly features in drugs and potential tracers for biomedical imaging with positron emission tomography (PET). Herein, we describe a rapid and transition metal-free conversion of fluoroform with paraformaldehyde into highly reactive potassium 2,2,2-trifluoroethoxide (CF 3 CH 2 OK) and demonstrate robust applications of this synthon in one-pot, two-stage 2,2,2-trifluoroethoxylations of both aromatic and aliphatic precursors. Moreover, we show that these transformations translate easily to fluoroform that has been labeled with either carbon-11 ( t 1/2 = 20.4 min) or fluorine-18 ( t 1/2 = 109.8 min), so allowing the appendage of complex molecules with a no-carrier-added 11 C- or 18 F- 2,2,2-trifluoroethoxy group. This provides scope to create candidate PET tracers with radioactive and metabolically stable 2,2,2-trifluoroethoxy moieties. We also exemplify syntheses of isotopologues of potassium 2,2,2-trifluoroethoxide and show their utility for stable isotopic labeling which can be of further benefit for drug discovery and development.

Isotopologue

10.1038/s41467-024-49975-7

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Citations (1)

Broad‐scope Syntheses of [¹¹C/¹⁸F]Trifluoromethylarenes from Aryl(mesityl)iodonium Salts

Chemistry - A European Journal (2023)

Sanjay Telu Susovan Jana Mohammad B. Haskali Bo Yeun Yang Jimmy E. Jakobsson

Efficient methods for labeling aryl trifluoromethyl groups to provide novel radiotracers for use in biomedical research with positron emission tomography (PET) are keenly sought. We report a broad-scope method for labeling trifluoromethylarenes with either carbon-11 (t

Synthon

10.1002/chem.202204004

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Citations (9)

Ligand-Based Virtual Screening as a Path to New Chemotypes for Candidate PET Radioligands for Imaging Tauopathies

Journal of Medicinal Chemistry (2024)

Bryan Hurtle Susovan Jana Lisheng Cai Victor W. Pike

Ligand-based virtual screening (LBVS) has rarely been tested as a method for discovering new structural scaffolds for PET radioligand development. This study used LBVS to discover potential chemotype leads for developing radioligands for PET imaging of tauopathies. ZINC12, a free database of over 12 million commercially available compounds, was searched to discover novel scaffolds based on similarities to four query compounds. Thirteen high-ranking hits were purchased and assayed for their ability to compete against three tritiated radioligands at their distinct binding sites in Alzheimer's disease brain tissue. Three hits were 2-substituted 6-methoxy naphthalenes. Synthetic elaboration of this new chemotype yielded three new ligands (

Chemotype

Radioligand

PET Imaging

10.1021/acs.jmedchem.4c00934

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Citations (2)

Development and Evaluation in Rat and Monkey of a Candidate Homochiral Radioligand for PET Studies of Brain Receptor Interacting Protein Kinase 1: [¹⁸F](S)-1-(5-(3-Fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2,2-dimethylpropan-1-one

ACS Chemical Neuroscience (2025)

Susovan Jana Mudasir Maqbool Xuefeng Yan Jimmy E. Jakobsson Adrian Lee

Receptor interacting protein kinase 1 (RIPK1) crucially upregulates necroptosis and is a key driver of inflammation. An effective PET radioligand for imaging brain RIPK1 would be useful for further exploring the role of this enzyme in neuroinflammation and for assisting drug discovery. Here, we report our progress on developing a PET radioligand for RIPK1 based on the phenyl-1

Radioligand

Radioligand Assay

10.1021/acschemneuro.4c00715

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[¹⁸F]SF51, a novel ¹⁸F-labeled PET radioligand for translocator protein 18kDa (TSPO) in brain, works well in monkeys but fails in humans

Journal of Cerebral Blood Flow & Metabolism (2024)

Xuefeng Yan Fabrice G. Siméon Jeih-San Liow Cheryl L. Morse Susovan Jana

[

Translocator protein

Radioligand

PET Imaging

10.1177/0271678x241304924

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Citations (0)