ResearchPad - natural-products https://www.researchpad.co Default RSS Feed en-us © 2020 Newgen KnowledgeWorks <![CDATA[The Biosynthesis of the Benzoxazole in Nataxazole Proceeds via an Unstable Ester and has Synthetic Utility]]> https://www.researchpad.co/article/N085c4db7-4156-4a3d-919a-5917dd39a86a Benzoxazole biosynthesis, a key step in the biosynthesis of the antitumor agent nataxazole, proceeds via a hemiorthoamide intermediate that arises from an unstable ester. NatL2 catalyzes the formation of this ester that spontaneously rearranges into an off‐pathway amide. In the presence of NatAM, the ester is converted to benzoxazole via a hemiorthoamide intermediate. These enzymes are used to synthesize a series of novel halogenated benzoxazoles.

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<![CDATA[Ellagic Acid, Kaempferol, and Quercetin from Acacia nilotica: Promising Combined Drug With Multiple Mechanisms of Action]]> https://www.researchpad.co/article/Nbd9646f3-1db7-4e84-a4f6-46261d9649ee

The pharmacological activity of Acacia nilotica’s phytochemical constituents was confirmed with evidence-based studies, but the determination of exact targets that they bind and the mechanism of action were not done; consequently, we aim to identify the exact targets that are responsible for the pharmacological activity via the computational methods. Furthermore, we aim to predict the pharmacokinetics (ADME) properties and the safety profile in order to identify the best drug candidates. To achieve those goals, various computational methods were used including the ligand-based virtual screening and molecular docking. Moreover, pkCSM and SwissADME web servers were used for the prediction of pharmacokinetics and safety. The total number of the investigated compounds and targets was 25 and 61, respectively. According to the results, the pharmacological activity was attributed to the interaction with essential targets. Ellagic acid, Kaempferol, and Quercetin were the best A. nilotica’s phytochemical constituents that contribute to the therapeutic activities, were non-toxic as well as non-carcinogen. The administration of Ellagic acid, Kaempferol, and Quercetin as combined drug via the novel drug delivery systems will be a valuable therapeutic choice for the treatment of recent diseases attacking the public health including cancer, multidrug-resistant bacterial infections, diabetes mellitus, and chronic inflammatory systemic disease.

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<![CDATA[Total Synthesis of the Schisandraceae Nortriterpenoid Rubriflordilactone A]]> https://www.researchpad.co/article/5b44dfb7463d7e40e68d76d1

Abstract

Full details of the total synthesis of the Schisandraceae nortriterpenoid natural product rubriflordilactone A are reported. Palladium‐ and cobalt‐catalyzed polycyclizations were employed as key strategies to construct the central pentasubstituted arene from bromoendiyne and triyne precursors. This required the independent assembly of two AB ring aldehydes for combination with a common diyne component. A number of model systems were explored to investigate these two methodologies, and also to establish routes for the installation of the challenging benzopyran and butenolide rings.

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<![CDATA[Short, Tin‐Free Synthesis of All Three Inthomycins]]> https://www.researchpad.co/article/5c61b99ad5eed0c48493cdf3

Abstract

The inthomycins are a family of structurally and biologically rich natural products isolated from Streptomyces species. Herein the implementation of a modular synthetic route is reported that has enabled the enantioselective synthesis of all three inthomycins. Key steps include Suzuki and Sonogashira cross‐couplings and an enantioselective Kiyooka aldol reaction.

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<![CDATA[Digging for biosynthetic dark matter]]> https://www.researchpad.co/article/5989daf5ab0ee8fa60bc2b02

An analysis of bacterial communities in soil samples from around the world reveals unexplored diversity in biosynthetic enzymes.

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