Practical Syntheses of (2<i>S</i>)‐R207910 and (2<i>R</i>)‐R207910

Chandrasekhar, Srivari; Babu, G. Suresh; Mohapatra, Debendra K.

doi:10.1002/ejoc.201001720

Cited by 25 publications

(22 citation statements)

References 24 publications

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“…BDQ was synthesized at CPRU, UKZN (Durban, South Africa) according to previously published methods 25 and its characterization was in keeping with that reported in literature. 26 BDQ D6 ( ref. 27 ) was employed as the internal standard (IS).…”

Section: Methodsmentioning

confidence: 99%

Bedaquiline has potential for targeting tuberculosis reservoirs in the central nervous system

et al. 2018

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Section: Methodsmentioning

confidence: 99%

Bedaquiline has potential for targeting tuberculosis reservoirs in the central nervous system

et al. 2018

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“…Synthesis of the mixed stereoisomers (2S) and (2R) of dehydro-tocotrienol beta (deh-T3β) was performed according to the procedure by Chandrasekhar et al [9] with minor modifications. We mixed 7 g of 2,5-dimethyl-1,4-benzoquinone in 25 mL ethanol and 35 mL diethyl ether.…”

Section: Synthesis Of Deh-t3βmentioning

confidence: 99%

Dehydro-Tocotrienol-β Counteracts Oxidative-Stress-Induced Diabetes Complications in db/db Mice

et al. 2021

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Hyperglycemia, hyperlipidemia, and adiposity are the main factors that cause inflammation in type 2 diabetes due to excessive ROS production, leading to late complications. To counteract the effects of increased free radical production, we searched for a compound with effective antioxidant properties that can induce coenzyme Q biosynthesis without affecting normal cellular functions. Tocotrienols are members of the vitamin E family, well-known as efficient antioxidants that are more effective than tocopherols. Deh-T3β is a modified form of the naturally occurring tocotrienol-β. The synthesis of this compound involves the sequential modification of geranylgeraniol. In this study, we investigated the effects of this compound in different experimental models of diabetes complications. Deh-T3β was found to possess multifaceted capacities. In addition to enhanced wound healing, deh-T3β improved kidney and liver functions, reduced liver steatosis, and improved heart recovery after ischemia and insulin sensitivity in adipose tissue in a mice model of type 2 diabetes. Deh-T3β exerts these positive effects in several organs of the diabetic mice without reducing the non-fasting blood glucose levels, suggesting that both its antioxidant properties and improvement in mitochondrial function are involved, which are central to reducing diabetes complications.

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“…Bedaquiline (TMC-207) was used as the internal standard (IS) (synthesised in our laboratory, its 1 H and 13 C NMR spectra corresponded to that in literature (Chandrasekhar et al 2011). All solvents were LC-MS grade and purchased from Sigma Aldrich (Steinham, Germany); Ultra-pure water was obtained using a Milli-Q water purification system (Bedford, MA, USA).…”

Section: Methodsmentioning

confidence: 99%

Neuroprotective potential of Linezolid: a quantitative and distribution study via mass spectrometry

et al. 2016

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A study was undertaken to determine the neuroprotective potential of Linezolid (LIN) in an animal model. Female Sprague-Dawley rats were either given a single (100 mg/kg) dose or treated daily for 4 weeks. A validated LC-MS/MS method was used to measure LIN levels in plasma and brain, this was paired with mass spectrometry imaging to determine the tissue spatial distribution of the drug. The results showed that after a single dose there was poor penetration of the drug into the brain. With multiple doses there were high tissue levels, with the drug reaching steady state in subsequent weeks. LIN displayed a promising distribution pattern with localisation in the brainstem. Systemic circulation is fed into the brain by the carotid and vertebral arteries which enter through the brain stem, therefore high drug concentrations is this area may protect against infectious agents entering via this route.

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Practical Syntheses of (2S)‐R207910 and (2R)‐R207910

Abstract: Concise and practical syntheses of (2S)-R207910 (3a) and (2R)-R207910 (3b) have been achieved in high overall yield of 12 % in 10 steps for each isomer starting from a known

Cited by 25 publications

References 24 publications

Bedaquiline has potential for targeting tuberculosis reservoirs in the central nervous system

Bedaquiline has potential for targeting tuberculosis reservoirs in the central nervous system

Dehydro-Tocotrienol-β Counteracts Oxidative-Stress-Induced Diabetes Complications in db/db Mice

Neuroprotective potential of Linezolid: a quantitative and distribution study via mass spectrometry

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