Synthese von 3-Amino-1.2-dithioliumsalzen und deren Umwandlung in 2-Nitro-3-amino-thiophene

Synthesis of 3-Amino-1,2-dithiolium Salts and their Conversion to 2-Nitro-3-aminothiophenes 3-Amino-1.2-dithiolium salts 2a–1 are easily available from 3-chloro-1,2-dithiolium salts 1 and secondary amines. A new procedure to prepare 2-nitro-3-aminothiophenes 3 starting from N,N-substituted 3-amino-5-phenyl-1,2-dithiolium salts 2 is described which consists in a nucleophilic exchange of a sulfur atom for the carbon atom of nitromethane. The structure of 3 has been confirmed by reductive cyclization and by spectroscopic methods.     

Targeting G Protein‐Coupled Receptors by Capture Compound Mass Spectrometry: A Case Study with Sertindole

Unbiased chemoproteomic profiling of small‐molecule interactions with endogenous proteins is important for drug discovery. For meaningful results, all protein classes have to be tractable, including G protein‐coupled receptors (GPCRs). These receptors are hardly tractable by affinity pulldown from lysates. We report a capture compound (CC)‐based strategy to target and identify GPCRs directly from living cells. We synthesized CCs with sertindole attached to the CC scaffold in different orientations to target the dopamine D2 receptor (DRD2) heterologously expressed in HEK 293 cells. The structure–activity relationship of sertindole for DRD2 binding was reflected in the activities of the sertindole CCs in radioligand displacement, cell‐based assays, and capture compound mass spectrometry (CCMS). The activity pattern was rationalized by molecular modelling. The most‐active CC showed activities very similar to that of unmodified sertindole. A concentration of DRD2 in living cells well below 100 fmol used as an experimental input was sufficient for unambiguous identification of captured DRD2 by mass spectrometry. Our new CCMS workflow broadens the arsenal of chemoproteomic technologies to close a critical gap for the comprehensive characterization of drug–protein interactions.     

DropsBox: the Dresden Open Software Toolbox

The Dresden Open Software Toolbox (DropsBox) is a software modelling toolbox consisting of a set of open source tools developed by the Software Technology Group at TU Dresden. The DropsBox is built on top of the Eclipse Platform and the Eclipse Modeling Framework. The DropsBox contributes to the development and application of domain-specific language changes (DSLs) in model-driven software development. It can be customised by tool and language developers to support various activities of a DSL’s life cycle ranging from language design to language application and evolution. In this paper, we provide an overview of the DSL life cycle, the DropsBox tools, and their interaction on a common example. Furthermore, we discuss our experiences in developing and integrating tools for DropsBox in an academic environment.     

Sustainable Intervention Plans for Igbo Cultural Region of Nigeria

The Igbos are one of the major tribes of Nigeria. Over the years, their distinct way of living have further accentuated their culture. The paper discusses the Igbo cultural landscape region which comprises of rural autonomous communities made up of clusters of kindred and villages. In spite of the existence of the townships serving as trade, political and administrative centers for more than one century, the rate of urbanization has been very slow thereby affecting the development of the communities physically, economically and socially at astonishing rates consuming farmlands and traditional community boundaries. This paper is aimed at creating awareness on the unique regional growth pattern in Igbo land heavily dependent on cultural and natural heritages for purpose of determining adaptable regional planning strategies for such vibrant cultural region. It has examined the key issues and suggested a way forward to a more sustainable development of the region.     

Cyclisierungen mit 1-Nitro-2-anilino-äthylenen

Cyclizations with 1-nitro-2-anilino-ethylenes The reaction of 1-nitro-2-anilino-2-methylthio-ethylenes 1 with oxalyl chloride yields the substituted 4-nitropyrrol-2,3-diones 4 , and with chlorocarbonyl-sulfenylchloride the 5-nitro-thiazolones 6 . The methylthio group from 6 can be exchanged by amines. From 1-nitro-2,2-bis(anilino)ethylenes 2 – available from 1-nitro-2,2-bis(methylthio)-ethylene and anilines – and the same reagents, the substituted 2-nitromethylene-imidazolidine-4,5-diones 5 and the thiazolo[4,5-d]thiazoledione 9 result. The condensation of 1-nitro-2-anilino-2-hydrazino-ethylene 3 with derivatives of carboxylic acids yields 2-nitromethyl-s-triazole 12 , with diacetyl the substituted 3-nitromethylene-as-triazine 13 .