Pharmacologically Active Phytomolecules Isolated from Traditional Antidiabetic Plants and Their Therapeutic Role for the Management of Diabetes Mellitus

Diabetes mellitus is a chronic complication that affects people of all ages. The increased prevalence of diabetes worldwide has led to the development of several synthetic drugs to tackle this health problem. Such drugs, although effective as antihyperglycemic agents, are accompanied by various side effects, costly, and inaccessible to the majority of people living in underdeveloped countries. Medicinal plants have been used traditionally throughout the ages to treat various ailments due to their availability and safe nature. Medicinal plants are a rich source of phytochemicals that possess several health benefits. As diabetes continues to become prevalent, health care practitioners are considering plant-based medicines as a potential source of antidiabetic drugs due to their high potency and fewer side effects. To better understand the mechanism of action of medicinal plants, their active phytoconstituents are being isolated and investigated thoroughly. In this review article, we have focused on pharmacologically active phytomolecules isolated from medicinal plants presenting antidiabetic activity and the role they play in the treatment and management of diabetes. These natural compounds may represent as good candidates for a novel therapeutic approach and/or effective and alternative therapies for diabetes.     

Acetylenic Replacement of Albicidin's Methacrylamide Residue Circumvents Detrimental E/Z Photoisomerization and Preserves Antibacterial Activity

The natural product albicidin is a highly potent inhibitor of bacterial DNA gyrase. Its outstanding activity, particularly against Gram-negative pathogens, qualifies it as a promising lead structure in the search for new antibacterial drugs. However, as we show here, the N-terminal cinnamoyl moiety of albicidin is susceptible to photochemical E/Z isomerization. Moreover, the newly formed Z isomer exhibits significantly reduced antibacterial activity, which hampers the development and biological evaluation of albicidin and potent derivatives thereof. Hence, we synthesized 13 different variants of albicidin in which the vulnerable para-coumaric acid moiety was replaced; this yielded photostable analogues. Biological activity assays revealed that diaryl alkyne analogues exhibited virtually undiminished antibacterial efficacy. This promising scaffold will therefore serve as a blueprint for the design of a potent albicidin-based drug.     

Mafsanalytische Bestimmung der Ferricyanwasserstoffs?ure bei Gegenwart von Ferri- und Cyanion

Ohne Zusammenfassung     

Einen Beitrag zur Methodik der Bestimmung von Keto-EnolGemisehen liefern

Ohne Zusammenfassung     

Nachweis und Bestimmung des Eisens, sowie seine Trennung von anderen Elementen

Ohne Zusammenfassung     

α-substituted Phosphoryl Compounds (I). The Crystal and Molecular Structure of Diethyl[5,6-dichloro-1,3-benzodioxol-(2)]-phosphonate,C11H13O5PCl2

Diethyl[5,6-dichloro- 1,3-benzodioxol-(2)]-phosphonate crystallizes in the triclinic space group P l̄ with two molecules per unit cell. The lattice parameters are a = 11.716 Å, b = 8.471 Å, c = 7.644 Å; α = 82.47° β = 95.81°, γ = 95.89°. With X-ray diffraction data collected on an automatic four circle diffractometer, the crystal structure was solved by direct methods and refined by least squares methods to an R value of 0.12 for 2374 measured reflections. The crystal used was im perfect. The substance is a derivative of acetales of formyl phosphoneacid esters. The aim is to find a correlation between the geometry of the structure and NMR data.     

Palladium-Catalyzed Arylation of Endocyclic 1-Azaallyl Anions: Concise Synthesis of Unprotected Enantioenriched cis-2,3-Diarylpiperidines

Unprotected cis-2,3-diarylpiperidines are synthesized through an unprecedented palladium-catalyzed cross-coupling reaction between aryl halides and elusive endocyclic 1-azaallyl anions. These intermediates are generated in situ by the deprotonation of 2-aryl-1-piperideines, precursors that are readily prepared in two operations from simple piperidines. An asymmetric version of this reaction with (2R, 3R)-iPr-BI-DIME as the ligand provides products in moderate to good yields and enantioselectivities. This study significantly expands the synthetic utility of endocyclic 1-azaallyl anions.     

Structures of Azomethine Imines of the Pyrazolidone-(3)-type (I). The Structure of 1-(4-Nitrobenzylidene-pyrazolidone-(3)-betaine

1-(4-Nitrobenzylidene)-pyrazolidone-(3)-betaine crystallizes in the orthorhombic space group Pbca with eight molecules per unit cell. The lattice parameters are a = 11.025 Å; b = 22.995 Å; c = 7. 677 Å. With X-ray diffraction data, collected on a automatical four circle diffractometer, the crystal structure was solved by direct methods and refined to an R-value of 0.047 for 1516 symmetrically independent reflections. The structure determination has been performed to contribute to the explanation of the photochromic behaviour of this special class of azomethine imines.