An alternative synthesis and X-ray crystallographic confirmation of (−)-stepholidine

Gadhiya, Satishkumar; Hu, Chunhua; Harding, Wayne W.

doi:10.1016/j.tetlet.2016.03.108

Cited by 6 publications

(4 citation statements)

References 16 publications

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“…Cocaine (a gift from NIDA) was dissolved in 0.9% saline to achieve a dose of 1 mg/kg/injection for the self-administration experiment. (−)-Stepholidine, synthesized as described previously (Gadhiya et al, 2016), was dissolved in distilled water and 10% dimethyl sulfoxide (DMSO) to achieve doses of 2.5, 5.0 and 10 mg/kg and was administered by IP injection.…”

Section: Methodsmentioning

confidence: 99%

(-)-Stepholidine reduces cue-induced reinstatement of cocaine seeking and cocaine self-administration in rats

Manuszak

Harding

Gadhiya

et al. 2018

Drug and Alcohol Dependence

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Section: Methodsmentioning

confidence: 99%

(-)-Stepholidine reduces cue-induced reinstatement of cocaine seeking and cocaine self-administration in rats

Manuszak

Harding

Gadhiya

et al. 2018

Drug and Alcohol Dependence

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“…As an impact, membrane fusion is essential for communication between membrane‐delineated compartments allowing the exchange of luminal contents or releasing their contents such as hormones and neurotransmitters into the extracellular milieu, or to deposit receptors and transporters to the membrane. [ 56–58 ] Homotypic fusion initiates the process to merge similar types of compartments such as endosome‐endosome fusion whereas the dissimilar type of compartments (for instance, synaptic vesicle exocytosis) can be fused in case of heterotypic fusion where latter fusion could be of central importance for development, repair of tissues and the pathogenesis of diseases. [ 54,57 ] During the membrane fusion process, the very first initiation required is to bring membranes of two fusing cells into proximity.…”

Section: Continuous Self‐assemblymentioning

confidence: 99%

Hierarchical Assemblies of Polymer Particles through Tailored Interfaces and Controllable Interfacial Interactions

Visaveliya

Köhler

2020

Adv Funct Materials

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Hierarchical assembly architectures of functional polymer particles are promising because of their physicochemical and surface properties for multi‐labeling and sensing to catalysis and biomedical applications. While polymer nanoparticles’ interior is mainly made up of the cross‐linked network, their surface can be tailored with soft, flexible, and responsive molecules and macromolecules as potential support for the controlled particulate assemblies. Molecular surfactants and polyelectrolytes as interfacial agents improve the stability of the nanoparticles whereas swellable and soft shell‐like cross‐linked polymeric layer at the interface can significantly enhance the uptake of guest nano‐constituents during assemblies. Besides, layer‐by‐layer surface‐functionalization holds the ability to provide a high variability in assembly architectures of different interfacial properties. Considering these aspects, various assembly architectures of polymer nanoparticles of tunable size, shapes, morphology, and tailored interfaces together with controllable interfacial interactions are constructed here. The microfluidic‐mediated platform has been used for the synthesis of constituents polymer nanoparticles of various structural and interfacial properties, and their assemblies are conducted in batch or flow conditions. The assemblies presented in this progress report is divided into three main categories: cross‐linked polymeric network's fusion‐based self‐assembly, electrostatic‐driven assemblies, and assembly formed by encapsulating smaller nanoparticles into larger microparticles.

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“…Akin to many scientific discoveries, AI in drug discovery has harbored healthy skepticism among the medicinal chemists. It is yet to be tested how AI can tackle the challenge of imbibing natural products to build synthetically feasible de novo designs as effective pharmacophores [ 67 , 68 ]. Also, the ventured chemical space has largely been small molecules; however, the advent of bio-conjugate therapies such as immunotherapy, RNAi therapeutics etc., where chemistry converges with biology is yet to be explored.…”

Section: Artificial Intelligence (Ai) In Drug Design and Molecularmentioning

confidence: 99%

Deep Learning in Drug Discovery and Medicine; Scratching the Surface

et al. 2018

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The practice of medicine is ever evolving. Diagnosing disease, which is often the first step in a cure, has seen a sea change from the discerning hands of the neighborhood physician to the use of sophisticated machines to use of information gleaned from biomarkers obtained by the most minimally invasive of means. The last 100 or so years have borne witness to the enormous success story of allopathy, a practice that found favor over earlier practices of medical purgatory and homeopathy. Nevertheless, failures of this approach coupled with the omics and bioinformatics revolution spurred precision medicine, a platform wherein the molecular profile of an individual patient drives the selection of therapy. Indeed, precision medicine-based therapies that first found their place in oncology are rapidly finding uses in autoimmune, renal and other diseases. More recently a new renaissance that is shaping everyday life is making its way into healthcare. Drug discovery and medicine that started with Ayurveda in India are now benefiting from an altogether different artificial intelligence (AI)—one which is automating the invention of new chemical entities and the mining of large databases in health-privacy-protected vaults. Indeed, disciplines as diverse as language, neurophysiology, chemistry, toxicology, biostatistics, medicine and computing have come together to harness algorithms based on transfer learning and recurrent neural networks to design novel drug candidates, a priori inform on their safety, metabolism and clearance, and engineer their delivery but only on demand, all the while cataloging and comparing omics signatures across traditionally classified diseases to enable basket treatment strategies. This review highlights inroads made and being made in directed-drug design and molecular therapy.

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An alternative synthesis and X-ray crystallographic confirmation of (−)-stepholidine

Abstract: A formal enantioselective synthesis of (−)-stepholidine that provides an alternative preparation of key lactone intermediate 2 is described. The stereostructure of (−)-stepholidine prepared via this method was confirmed by x-ray diffraction.

Cited by 6 publications

References 16 publications

(-)-Stepholidine reduces cue-induced reinstatement of cocaine seeking and cocaine self-administration in rats

(-)-Stepholidine reduces cue-induced reinstatement of cocaine seeking and cocaine self-administration in rats

Hierarchical Assemblies of Polymer Particles through Tailored Interfaces and Controllable Interfacial Interactions

Deep Learning in Drug Discovery and Medicine; Scratching the Surface

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