Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors

Banerjee, Abhisek; Narayana, Lakshminarayana; Raje, Firoj; Pisal, Dnyandeo; Kadam, Pradip A.; Gullapalli, Srinivas; Kumar, Hemant; More, Sandeep Vasant; Bajpai, Malini; Sangana, Ramachandra; Jadhav, Satyawan B.; Gudi, Girish; Khairatkar-Joshi, Neelima; Merugu, Ravi R.T.; Voleti, Sreedhara R.; Gharat, Laxmikant A.

doi:10.1016/j.bmcl.2013.10.027

Cited by 24 publications

(23 citation statements)

References 34 publications

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“…12 Such heterocyclization provides a novel way for the synthesis of benzo[5, 1-b]imidazothiazoles, which have a wide application in the drug design. 19 The described methods of benzo[5, 1-b]imidazothiazoles avoids the use of metal-based catalysts, 19,20 and appears open an interesting path towards heteroatomdoped polycyclic aromatics.…”

Section: Scheme 1 Synthesis Of Benzomentioning

confidence: 99%

Preparation and Synthetic Applicability of Novel Imidazole-Containing Cyclic Iodonium Salts

Nikita¹,

Vlasenko²,

Yoshimura³

et al. 2021

Preprint

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The novel approach to the preparation of imidazole-substituted cyclic iodonium salts has been developed via oxidative cyclization of 1-phenyl-5-iodoimidazole using cheap and available Oxone®/H2SO4 oxidative system. The structure of newly prepared compounds has been proved by X-ray monocrystal diffractometry revealing the characteristic surface features for cyclic iodonium salts. The prepared compounds demonstrated the high reactivity in the heterocyclization reactions with elemental sulfur affording benzo[5,1-b]imidazothiazoles with good yields.

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Section: Scheme 1 Synthesis Of Benzomentioning

confidence: 99%

Preparation and Synthetic Applicability of Novel Imidazole-Containing Cyclic Iodonium Salts

Nikita¹,

Vlasenko²,

Yoshimura³

et al. 2021

Preprint

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“…Inhibiting PDE10A was shown to have a positive regulatory effect on basal ganglia function, making it a potential target for the treatment of psychosis, Parkinsonism and Schizophrenia [32,303,307,308]. PDE10 inhibition by Papaverine improved spatial and object recognition memory and significantly increased pGluA1 and pCREB levels in the hippocampus when studied in R6/1 mice, suggesting the utilization of PDE10 inhibitors as a therapeutic strategy for the treatment of HD [309].…”

Section: The Utility Of Pde Inhibitors For Neuroprotection and Neumentioning

confidence: 99%

Phosphodiesterase Inhibitors as a Therapeutic Approach to Neuroprotection and Repair

Knott

Assi

Rao

et al. 2017

IJMS

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A wide diversity of perturbations of the central nervous system (CNS) result in structural damage to the neuroarchitecture and cellular defects, which in turn are accompanied by neurological dysfunction and abortive endogenous neurorepair. Altering intracellular signaling pathways involved in inflammation and immune regulation, neural cell death, axon plasticity and remyelination has shown therapeutic benefit in experimental models of neurological disease and trauma. The second messengers, cyclic adenosine monophosphate (cyclic AMP) and cyclic guanosine monophosphate (cyclic GMP), are two such intracellular signaling targets, the elevation of which has produced beneficial cellular effects within a range of CNS pathologies. The only known negative regulators of cyclic nucleotides are a family of enzymes called phosphodiesterases (PDEs) that hydrolyze cyclic nucleotides into adenosine monophosphate (AMP) or guanylate monophosphate (GMP). Herein, we discuss the structure and physiological function as well as the roles PDEs play in pathological processes of the diseased or injured CNS. Further we review the approaches that have been employed therapeutically in experimental paradigms to block PDE expression or activity and in turn elevate cyclic nucleotide levels to mediate neuroprotection or neurorepair as well as discuss both the translational pathway and current limitations in moving new PDE-targeted therapies to the clinic.

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“…Rolipram was active in the sensorimotor gating test [31] which may be explained by the enhanced DARPP-32 phosphorylation invoked by D1 receptor activation in the frontal cortex. Recent translational studies of PDE have also focused attention on PDE-10 and PDE-2A as putative targets for pro-cognitive strategy in SCZ and neurodegenerative disorders: Alzheimer dementia [33,34]. None of the PDE -10A or PDE-2 is in Phase II/III clinical trials in SCZ.…”

Section: Disc-1 Gene and Pde: Role In Schizophreniamentioning

confidence: 99%

Exploring Standardized Zembrin® Extracts from the South African plant Sceletium tortuosum in Dual Targeting Phosphodiesterase-4 (PDE-4) and Serotonin Reuptake Inhibition as potential treatment in Schizophrenia

Chiu¹

2017

IJCAM

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Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors

Cited by 24 publications

References 34 publications

Preparation and Synthetic Applicability of Novel Imidazole-Containing Cyclic Iodonium Salts

Preparation and Synthetic Applicability of Novel Imidazole-Containing Cyclic Iodonium Salts

Phosphodiesterase Inhibitors as a Therapeutic Approach to Neuroprotection and Repair

Exploring Standardized Zembrin® Extracts from the South African plant Sceletium tortuosum in Dual Targeting Phosphodiesterase-4 (PDE-4) and Serotonin Reuptake Inhibition as potential treatment in Schizophrenia

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