Mixed dialkyltin(IV) trifluoroacetates

Mixed dialkytin(IV) trifluoroacetates,Me EtSn(O₂CCF₃)₂,Et Pr ⁿ Sn(O₂CCF₃)₂ andPr ⁿ Bu ⁿ Sn(O₂CCF₃)₂ have been prepared by metathetical reactions of the corresponding dialkyltin(IV) chlorides with silver trifluoroacetate in CH₂Cl₂. They are monomeric in benzene and nonconducting inMeNO₂ andMeCN. Bidentate trifluoroacetate groups are indicated by their IR spectra.Mössbauer spectra confirmtrans-arrangement of theR-Sn-R moiety.¹H,¹⁹F NMR and mass spectra are also discussed.

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Gemischte Dialkylzinn(IV)-trifluoracetate

Zusammenfassung Die gemischten Dialkylzinn(IV)-trifluoroacetateMe EtSn(O₂CCF₃)₂,Et Pr ⁿ Sn(O₂CCF₃)₂ undPr ⁿ Bu ⁿ Sn(O₂CCF₃)₂ wurden über Metathese-Reaktionen der entsprechenden Dialkylzinn(IV)-chloride mit Silbertrifluoracetat in CH₂Cl₂ dargestellt. Sie sind monomer in Benzol und nichtleitend inMeNO₂ undMeCN. Die IR-Spektren zeigen zweizähnige Trifluoracetat-Gruppen an. DieMössbauer-Spektren bestätigen dietrans-Anordnung derR-Sn-R-Einheit. Die¹H-,¹⁹F-NMR und die Massenspektren werden ebenfalls diskutiert.

     

Stereoselective synthesis of (−)-allosedamine

A stereoselective synthesis of (−)-allosedamine is disclosed. β-Aminosulfoxide 4 was generated stereoselectively by condensation of the sulfinyl anion 2 with N-Ts imine 3. The bromohydrin 5 was obtained by intramolecular sulfinyl group participation and the piperidine ring of allosedamine was elaborated using the ring-closing metathesis (RCM) reaction.     

A simple stereocontrolled synthesis of salinosporamide A

A simple and effective stereocontrolled synthesis of salinosporamide A has been developed. This process, the first synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. Salinosporamide A was of special interest as a synthetic target because of its potent in vitro cytotoxic activity against many tumor cell lines (IC(50) values of 10 nM or less).     

Advanced Drug Delivery Micro- and Nanosystems for Cardiovascular Diseases

Advanced drug delivery micro- and nanosystems have been widely explored due to their appealing specificity/selectivity, biodegradability, biocompatibility, and low toxicity. They can be applied for the targeted delivery of pharmaceuticals, with the benefits of good biocompatibility/stability, non-immunogenicity, large surface area, high drug loading capacity, and low leakage of drugs. Cardiovascular diseases, as one of the primary mortalities cause worldwide with significant impacts on the quality of patients’ life, comprise a variety of heart and circulatory system pathologies, such as peripheral vascular diseases, myocardial infarction, heart failure, and coronary artery diseases. Designing novel micro- and nanosystems with suitable targeting properties and smart release behaviors can help circumvent crucial challenges of the tolerability, low stability, high toxicity, and possible side- and off-target effects of conventional drug delivery routes. To overcome different challenging issues, namely physiological barriers, low efficiency of drugs, and possible adverse side effects, various biomaterials-mediated drug delivery systems have been formulated with reduced toxicity, improved pharmacokinetics, high bioavailability, sustained release behavior, and enhanced therapeutic efficacy for targeted therapy of cardiovascular diseases. Despite the existing drug delivery systems encompassing a variety of biomaterials for treating cardiovascular diseases, the number of formulations currently approved for clinical use is limited due to the regulatory and experimental obstacles. Herein, the most recent advancements in drug delivery micro- and nanosystems designed from different biomaterials for the treatment of cardiovascular diseases are deliberated, with a focus on the important challenges and future perspectives.     

Antibacterial and wound healing activities of silver nanoparticles embedded in cellulose compared to other polysaccharides and protein polymers

Cellulose - The aggregation of silver nanoparticles (AgNPs) in colloidal solution and the oxidative cytotoxicity towards human cells are two major hindrances for their thriving medicinal...     

L‐Proline–H2O2: A New Chemoselective Approach for Oxidation of Sulfides to Sulfoxides

A facile and selective oxidation of sulfides to sulfoxides using an L‐proline–H₂O₂ system for structurally divergent sulfide substrates with excellent yields at ambient conditions is reported.     

Micellar Mediated Halodecarboxylation of α,β‐Unsaturated Aliphatic and Aromatic Carboxylic Acids—A Novel Green Hunsdiecker–Borodin Reaction

A Novel Hunsdiecker‐Borodin reaction (HBR) has been carried out efficiently with α,β‐unsaturated aliphatic and aromatic carboxylic acids by using N‐halo succinimides such as N‐chloro succinimide (NCS), N‐bromo succinimide (NBS), and N‐iodo succinimide (NIS) under micellar media. The reaction with α,β‐unsaturated aromatic carboxylic acids afforded β‐halo styrenes in excellent yield while α,β‐unsaturated aliphatic carboxylic acids underwent decarboxylation and to give corresponding halo derivatives. The reactions are dramatically accelerated in micellar media. This procedure works efficiently in CTAB (cetyl trimethyl ammonium bromide), SDS (sodium dodecyl sulfate), and TX (Triton‐X‐100) media under stirred conditions at room temperature. At reflux temperatures the yield of reaction products were further enhanced from good to excellent.     

Targeting tribbles homolog 3 (TRIB3) protein against type 2 diabetes for the identification of potential inhibitors by in silico screening

Tribbles homolog 3 (TRIB3) protein is inhibiting the insulin signaling by directly binding to the Akt/PKB leading to insulin resistance in the pancreas causing type 2 diabetes mellitus. Hence, TRIB3 protein is considered as a possible drug target for the new lead identification against type 2 diabetes. In the present study, the homology model of TRIB3 protein was generated to explore its biochemical function and molecular interactions in the new lead identification. The energy minimization of TRIB3 protein was carried out and evaluated by validation protocols for structure reliability. The druggable binding site of TRIB3 protein was identified for the virtual screening and molecular docking studies. The Asinex-fragments library of 22634 small molecules was docked at TRIB3 active site using the Glide module to identify new chemical entities. A total of 9 molecules were identified as final hits from virtual screening and their potency was ranked using Glide score, Glide energies, and residues interactions. The 6 prioritized lead molecules were further optimized using AutoDock, Prime MM/GBSA, and percentage of human oral absorption for the identification of potential leads. The molecules L2, L5, and L6 are identified as lead inhibitors and are showing consistent interactions with key residues Glu194 and Lys196 of TRIB3 protein. The identified potential leads were analyzed by ADME properties for their drug likeness and HergIC50 values are predicted for the prevention of preclinical failures. The present work sheds light on the identification of the best lead molecules against TRIB3 protein and offers a route to design as novel potential drug candidates for T2DM.     

A Convenient Reduction of α,β-Unsaturated Nitroalkenes to Alkylamines Using Boron Hydrides

α,β-Unsaturated nitroalkenes are reduced to alkylamines in good yields by excess of borane-THF in presence of catalytic amount of sodium borohydride.