Methyl imidazo[1,2-b]pyridazine-2-carbamates and related compounds as potential antifilarial agents

A series of imidazo[1,2-b]pyridazines have been synthesized for antifilarial evaluation. The compounds prepared include methyl 6-benzoylimidazo[1,2-b]pyridazine-2-carbamate ( 12 ), 6-benzoyl-2-t-butylimidazo[1,2-b]pyridazine ( 13 ), methyl 6-(4-fluorobenzoyl)imidazo[1,2-b]pyridazine-2-carbamate ( 14 ), and methyl 6-(2-thienylcarbonylcarbonyl)imidazo[1,2-b]pyridazine-2-carbamate ( 15 ) which are aza analogs of the anthelmintic agents mebendazole, flubendazole and nocadazole. In addition, the preparation of a series of 2-t-butylimidazo[1,2-b]-pyridazine-6-carboxylic acid derivatives is described. Electrophilic bromination and iodination substitutions of 2-t-butyl-6-methylimidazo[1,2-b]pyridazine afforded 3-halo derivatives. Methyl 6-(4-fluorobenzoyl)pyridazine-3-carbamate was also prepared for antifilarial evaluation. None of these compounds possessed significant antifilarial activity against Brugia pahangi or Acanthocheilonema viteae infections in jirds.     

Synthesis of 4,5-dihydro-1H,3H-thieno[3,4-c]thiophene and 4,5-dihydro-1H,3H-thieno[3,4-c]furan

4,5-Dihydro-1H,3H-thieno[3,4-c]thiophene and 4,5-dihydro-1H,3H-thieno[3,4-c]furan were synthesized by retro Diels-Alder reactions under flash vacuum thermolysis conditions.     

A cluster of many small holes with negative imaginary surface impedances may generate a negative refraction index

We deal with the scattering of an acoustic medium modeled by an index of refraction n varying in a bounded region Ω of and equal to unity outside Ω. This region is perforated with an extremely large number of small holes D_m's of maximum radius a, a << 1, modeled by surface impedance functions. Precisely, we are in the regime described by the number of holes of the order M:=O(a^{β ? 2}), the minimum distance between the holes is d ～ a^t, and the surface impedance functions of the form λ_m～λ_m,0a^?β with β > 0 and λ_m,0 being constants and eventually complex numbers. Under some natural conditions on the parameters β,t, and λ_m,0, we characterize the equivalent medium generating approximately the same scattered waves as the original perforated acoustic medium. We give an explicit error estimate between the scattered waves generated by the perforated medium and the equivalent one, respectively, as a→0. As applications of these results, we discuss the following findings:

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Ultrafast Click Chemistry with Fluorosydnones

We report the synthesis and reactivity of 4‐fluorosydnones, a unique class of mesoionic dipoles displaying exquisite reactivity towards both copper‐catalyzed and strain‐promoted cycloaddition reactions with alkynes. Synthetic access to these new mesoionic compounds was granted by electrophilic fluorination of σ‐sydnone Pd^II precursors in the presence of Selectfluor. Their reactions with terminal and cyclic alkynes were found to proceed very rapidly and selectively, affording 5‐fluoro‐1,4‐pyrazoles with bimolecular rate constants up to 10⁴ m ^?1 s^?1, surpassing those documented in the literature with cycloalkynes. Kinetic studies were carried out to unravel the mechanism of the reaction, and the value of 4‐fluorosydnones was further highlighted by successful radiolabeling with [¹⁸F]Selectfluor.     

Targeted borate complex formation as followed with electrospray ionization Fourier transform ion cyclotron mass spectrometry: monomolecular model system and polyborate formation

Fourier transform ion cyclotron resonance mass spectrometry (FTICR-MS) was applied to identify boric acid(B degrees)/borate(B-) complexes in a monomolecular model system, composed of aqueous caffeic acid and boric acid/borate solutions in various concentration ratios at pH 9.2. Using negative mode electrospray ionization as a 'soft' ionization technique, clusters of polyborate were detected beside the well-known BL degrees , BL- and BL2- complexes. An algorithm for the detection of boron complexes, based on their accurate mass and isotope patterns, is proposed which enabled the assignment of elemental compositions/structural formulae of boron/ligand complexes. We present experimental evidence of self-oligomerization of up to six borate units with caffeic acid, resulting in stable covalently bound polyborate-polyol complexes.     

Jacobi polynomials from compatibility conditions

We revisit the ladder operators for orthogonal polynomials and re-interpret two supplementary conditions as compatibility conditions of two linear over-determined systems; one involves the variation of the polynomials with respect to the variable (spectral parameter) and the other a recurrence relation in (the lattice variable). For the Jacobi weight

we show how to use the compatibility conditions to explicitly determine the recurrence coefficients of the monic Jacobi polynomials.

     

Synthesis,antibacterial activity,and fluorescence properties of a novel series from [2,4-dioxochromen-3(4<Emphasis Type="Italic">H</Emphasis>)methyl]amino acid

A new solvent-free method for synthesis of starting compounds 2,4-dioxochromen-3(4H)methyl amino acetic acid derivatives 1a–e via a green approach is reported. Also, the behavior of compound 1a towards various nitrogen nucleophiles such as primary amines, hydrazine hydrate, and hydroxylamine hydrochloride to give corresponding compounds 2–4 was studied. Furthermore, chlorination of compound 1a using a mixture of PCl₅/POCl₃ to yield acid chloride derivative 5 and the reaction of the latter compound 5 with various amino acids to obtain dipeptide compounds 6a–e are described. Moreover, cyclization of compound 1a in alkaline medium to afford dihydrochromeno[3,4-c]pyrrole-1-carboxylic acid 7 and cyclization of 6b in acidic medium, namely Ac₂O, to yield piperazine derivative 8 are reported. Also, reaction of compound 1a with maleic anhydride in dioxane to afford Diels–Alder adduct 9, which posteriorly reacted with hydrazine hydrate to give 10, was investigated. Most of the newly synthesized compounds were screened against Gram-positive and Gram-negative bacteria, with compound 5 exhibiting the maximum inhibition zone towards all four types of bacteria. In addition, the absorption and fluorescence emission of some of the substituted coumarins were studied in dioxane, revealing that the substituents altered both the absorption and fluorescence emission maxima.     

Hybrid Wireless Sensors Deployment Scheme with Connectivity and Coverage Maintaining in Wireless Sensor Networks

With the rapid growth of the internet of things (IoT), an impressive number of IoT’s application based on wireless sensor networks (WSNs) has been deployed in various domain. Due to its wide ranged applications, WSNs that have the capability to monitor a given sensing field, became the most used platform of IoT. Therefore, coverage becomes one of the most important challenge of WSNs. The search for better positions to assign to the sensors in order to control each point of an area of interest and the collection of data from sensors are major concerns in WSNs. This work addresses these problems by providing a hybrid approach that ensures sensors deployment on a grid for targets coverage while taking into account connectivity. The proposed sequential hybrid approach is based on three algorithms. The first places the sensors so as to all targets are covered. The second removes redundancies from the placement algorithm to reduce the number of sensors deployed. The third one, based on the genetic algorithm, aims to generate a connected graph which provide a minimal path that links deployed sensors and sink. Simulations and a comparative study were carried out to prove the relevance of the proposed method.