An efficient two-step synthesis of 3-allylindoles

A two-step synthetic sequence for an efficient synthesis of 3-allylindoles is described.     

A short and efficient synthesis of furo[2,3-b]indoles

Application of Wittig olefination-Claisen rearrangement protocol for the short synthesis of furo[2,3-b]indoles is described.     

Fly ash supported NiO as an efficient catalyst for the synthesis of xanthene and its molecular docking study against plasmodium glutathione reductase

A novel fly ash supported NiO (FA–NiO) nanocomposite solid heterogeneous catalyst has been prepared by impregnation of Ni(NO₃)₂ · 6H₂O on thermally activated fly ash (FA) support. FT-IR spectroscopy, X-ray diffraction analysis, scanning electron microscopy, TEM and BET techniques were employed to characterize the catalyst. The catalytic adeptness of FA–NiO was tested and optimized in xanthene formation. Catalyst gave very high yield and good purity. Stability of the catalyst could be promising as it easily recovered and reused giving a similar yield up to four cycles. FA–NiO is an efficient catalyst providing an environmentally clean process for xanthene formation and for developing a revolutionary way to use the majority of waste fly ash. Further, we have also performed docking simulation between 1ONF and a xanthene molecule to evaluate binding orientation and affinity of the ligand.     

Phosphine-free Pd-salen complexes as efficient and inexpensive catalysts for Heck and Suzuki reactions under aerobic conditions

Phosphine-free palladium-salen complexes, N,N′-bis(salicylidene)-ethylenediamino-palladium and N,N′-bis(salicylidene)-1,2-phenylenediamino palladium, are found to be highly active catalysts for the Heck olefination of aryl iodides and Suzuki reaction of aryl iodides and bromides giving excellent yields (70-90%) of products under aerobic conditions, in short reaction times (10-60 min).     

Tracer diffusion of Co2+ ions in agar gel containing multi-electrolyte systems

Tracer diffusion coefficients of cobalt ions have been measured in the supporting medium containing multi-electrolyte systems of alkali bromides. The electrolyte concentration was varied between 10^–6-0.1M at 25°C and the diffusion coefficients were determined by zone-diffusion technique using agar gel medium. The trend in the theoretical values of diffusion coefficients is accounted for by considering the relative contribution of mobility function, ionic strength as well as ion size parameter to the theoretical value in different systems. While the deviations between theoretical and experimental values of diffusion coefficients are explained on the basis of various co-occurring effects in ion-gel-water system.     

Composite representation invariants and unoriented topological string amplitudes

Sinha and Vafa [1] had conjectured that the SO   Chern–Simons gauge theory on S³$S^3$ must be dual to the closed A  -model topological string on the orientifold of a resolved conifold. Though the Chern–Simons free energy could be rewritten in terms of the topological string amplitudes providing evidence for the conjecture, we needed a novel idea in the context of Wilson loop observables to extract cross-cap c=0,1,2$c=0,1,2$ topological amplitudes. Recent paper of Marino [2] based on the work of Morton and Ryder [3] has clearly shown that the composite representation placed on the knots and links plays a crucial role to rewrite the topological string cross-cap c=0$c=0$ amplitude. This enables extracting the unoriented cross-cap c=2$c=2$ topological amplitude. In this paper, we have explicitly worked out the composite invariants for some framed knots and links carrying composite representations in U(N)$U(N)$ Chern–Simons theory. We have verified generalised Rudolph's theorem, which relates composite invariants to the invariants in SO(N)$\mathit{SO}(N)$ Chern–Simons theory, and also verified Marino's conjectures on the integrality properties of the topological string amplitudes. For some framed knots and links, we have tabulated the BPS integer invariants for cross-cap c=0$c=0$ and c=2$c=2$ giving the open-string topological amplitude on the orientifold of the resolved conifold.     

Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides

The inhibition of insulin-regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV is known to improve memory and learning in rats. Screening 10 500 low-molecular-weight compounds in an enzyme inhibition assay with IRAP from Chinese Hamster Ovary (CHO) cells provided an arylsulfonamide (N-(3-(1H-tetrazol-5-yl)phenyl)-4-bromo-5-chlorothiophene-2-sulfonamide), comprising a tetrazole in the meta position of the aromatic ring, as a hit. Analogues of this hit were synthesized, and their inhibitory capacities were determined. A small structure–activity relationship study revealed that the sulfonamide function and the tetrazole ring are crucial for IRAP inhibition. The inhibitors exhibited a moderate inhibitory potency with an IC₅₀=1.1±0.5 μm for the best inhibitor in the series. Further optimization of this new class of IRAP inhibitors is required to make them attractive as research tools and as potential cognitive enhancers.     

Wittig Olefination–Claisen Rearrangement Protocol for Cyclohexene Annulation

A two-step iterative sequence of Wittig olefination followed by Claisen rearrangement resulted in 1,7-octadienes, which afforded the corresponding cyclohexene carbaldehydes upon ring-closing metathesis with Grubbs catalyst.     

NO-NSAIDs. Part 3: nitric oxide-releasing prodrugs of non-steroidal anti-inflammatory drugs

In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, sulindac, ibuprofen and indomethacin. These prodrugs have NO-releasing disulfide linker attached to a parent NSAID via linkages such as an ester (compounds 9-16), a double ester (compounds 17-24), an imide (compounds 25-30) or an amide (compounds 31-33). Among these NO-NSAIDs, the ester-containing NO-aspirin (9), NO-diclofenac (10), NO-naproxen (11), and the imide-containing NO-aspirin (25), NO-flurbiprofen (27) and NO-ketoprofen (28) have shown promising oral absorption, anti-inflammatory activity and NO-releasing property, and also protected rats from NSAID-induced gastric damage. NO-aspirin compound 25, on further co-evaluation with aspirin at equimolar doses, exhibited comparable dose-dependent pharmacokinetics, inhibition of gastric mucosal prostaglandin E(2) (PGE(2)) synthesis and analgesic properties to those of aspirin, but retained its gastric-sparing properties even after doubling its oral dose. These promising NO-NSAIDs could therefore represent a new class of potentially "Safe NSAIDs" for the treatment of arthritic pain and inflammation.