Synthesis and Antiproliferative Activity of Novel Hydrazono Thiazolidene and Thiazole Derivatives Bearing Rhodanine Moiety

Russian Journal of General Chemistry - Some new fluoro-heterocyclic compounds containing thiazole and pyridine moities have been synthesized and studied for their antiproliferative activity....     

Heterocyclic synthesis via enaminones: Novel synthesis of (1H)‐pyridin‐2‐one,pyrazolo[1,5‐a]pyrimidine and isoxazole derivatives incorporating a N‐methylphthalimide and their biological evaluation

Novel synthesis of (1H)‐pyridin‐2‐one, pyrazolo[1,5‐a]pyrimidine and isoxazole derivatives incorporating N‐methylphthalimide moiety are reported. Reaction of enaminone 2 with malononitrile affords 4. Condensation of 2 with cyanothioacetamide or benzoylacetonitrile affords compounds 6 and 7 respectively. Reaction of 2 with hydrazine hydrate afford 2,3‐dihydrophthalazine‐1,4‐dione ( 10 ). Condensation of 2 with hydroxylamine and 3‐aminopyrazole derivatives affords compounds 12 and 15a,b respectively. Antimicrobial and antifungal activity were determined for representative compounds and most of them showed moderate activity as antimicrobial agents, while compounds 2 and 7 show strong activity against Aspergillus niger. The structure of the newly synthesized compounds was elucidated by elemental analyses and ¹H nmr spectra and some cases by ¹³C nmr investigation.     

Synthesis of Some Novel 2‐Anilinothiophene, 2,3′‐Bithienyl and Thienylthiopyridine Derivatives Resistance to Penicillium Digitatum Effect the Fruit

Reaction of benzotriazol‐1‐yl acetone 1 with phenyl isothiocyanate followed with α‐chloroacetone or ethyl‐α‐chloroacetate afforded 2‐anilinothiophenes 3 or 4 , respectively. Treatment of 3 with malononitrile at different reaction conditions afforded 6 or 7 . Reaction of 1 with CS₂ in DMF and phenacylbromide afforded S‐alkylated thiophene 10 . Reactions of the latter compound with different active methylene nitriles afforded thienylthiopyridine derivatives 14 and 15 . Condensation of 10 with hydrazine hydrate afforded hydrazon derivative 16 . Reaction of thiophene 17 with formamide in DMF afforded 19 which converted to N‐thienylpyrimidine 20 when treated with malononitrile. The structure of the newly synthesized compounds has been established on the basis of their analytical and spectral data. The compounds were also investigated for antibacterial and antifungal activities.     

Simultaneous Kinetic‐Spectrophotometric Determination of Hydrazine and its Derivatives by Partial Least Squares and Principle Component Regression Methods

Simultaneous kinetic‐spectrophotometric determination of a ternary mixture of hydrazine (HZ) and its derivatives by principal component regression (PCR) and partial least squares (PLS) calibration is described. The methods were based on the difference observed in the reduction rate of iron(III) with HZ, thiosemicarbazide (TSCZ) and phenylhydrazine (PHZ) in the presence of 2,2′‐bipyridine (Bpy). The colored complex of [Fe(Bpy)₃]²⁺ was formed in sodium dodecyl sulfate (SDS) as micellar media, and then monitored at 520 nm. The results showed that simultaneous determination of HZ, TSCZ and PHZ could be performed in their concentration ranges of 1.0–70.0, 0.2–6.0 and 0.1–10.0 μg mL^?1, respectively. The root mean squares errors of prediction (RMSEP) of HZ, TSCZ and PHZ were 0.719, 0.164 and 0.105 (for PLS) 0.788, 0.166 and 0.993 (for PCR), respectively. Both methods (PCR and PLS) were validated using a set of synthetic sample mixtures and then applied for simultaneous determination of HZ, TSCZ and PHZ in water samples.     

Influence of radiation on cation exchange reactions and electrical conductivity behavior of H-Mordenites

The transport of hydrochloric acid across a supported liquid membrane using Aliquat 336 in xylene as a carrier was studied. The effect of carrier concentration (0.1–0.6M) on the transportation of hydrochloric acid with and without phase modifier was investigated. The study indicated that the flux of transportation decreased with increasing carrier concentration in the absence of phase modifier. In the presence of phase modifier, however, the flux increased up to 0.2M carrier concentration and started decreasing afterwards. The transportation behavior of hydrochloric acid with and without phase modifier has been attributed to the tendency of aggregation of the carrier.     

Methylated Azopyridine as a New Electron Transfer Mediator for the Electrocatalytic Oxidation of NADH

Carbon ionic liquid electrode (CILE) has been modified with a new synthesized mediator i.e. N,N′‐dimethyl‐4,4′‐azopyridinium hexafluorophosphate (MAZPHP) via sol process and the electron transfer mediating characteristics of this mediator has been evaluated. 4,4′‐Azopyridine (AZP) did not show any electrocatalytic activity toward the selected probe, NADH, while its synthesized methylated derivative, MAZPHP, is a very efficient mediator for the electrocatalytic NADH oxidation. Cyclic voltammetry of MAZPHP/Sol/CILE exhibited a pair of reversible peaks corresponding to incorporated mediator with a formal potential of about 221 mV vs. Ag/AgCl. MAZPHP/Sol/CILE is free from fouling effects by the oxidation products of NADH which generally give hindrance to amperometric detection of NADH. Using amperometric technique, NADH can be determined in the range of 1.0×10^?5 M to 1.4×10^?3 M with a detection limit of 2.0×10^?6 M.     

Empirical analysis of self-adaptive differential evolution

Differential evolution (DE) is generally considered as a reliable, accurate, robust and fast optimization technique. DE has been successfully applied to solve a wide range of numerical optimization problems. However, the user is required to set the values of the control parameters of DE for each problem. Such parameter tuning is a time consuming task. In this paper, a self-adaptive DE (SDE) algorithm which eliminates the need for manual tuning of control parameters is empirically analyzed. The performance of SDE is investigated and compared with other well-known approaches. The experiments conducted show that SDE generally outperform other DE algorithms in all the benchmark functions. Moreover, the performance of SDE using the ring neighborhood topology is investigated.     

Phototherapeutic Effect of Low‐Level Laser on Thyroid Gland of Gamma‐Irradiated Rats

One inescapable feature of life on the earth is exposure to ionizing radiation. The thyroid gland is one of the most sensitive organs to gamma‐radiation and endocrine disrupters. Low‐level laser therapy (LLLT) has been used to stimulate tissue repair, and reduce inflammation. The aim of this study was to gauge the value of using Helium–Neon laser to repair the damaged tissues of thyroid gland after gamma‐irradiation. Albino rats were used in this study (144 rats), divided into control, gamma, laser, and gamma plus laser‐irradiated groups, each group was divided into six subgroups according to time of treatment (total six sessions). Rats were irradiated once with gamma radiation (6 Gy), and an external dose of laser (Wavelength 632.8 nm, 12 mW, CW, Illuminated area 5.73 cm², 2.1 mW cm^?2, 120 s, 1.4 J, 0.252 J cm^?2) twice weekly localized on thyroid region of the neck, for a total of six sessions. Animals were sacrificed after each session. Analysis included thyroid function, oxidative stress markers, liver function and blood picture. Results revealed improvement in thyroid function, liver function and antioxidant levels, and the blood cells count after LLLT.     

Studies and X‐ray Determinations with 2‐(Acetonylthio)benzothiazole: Synthesis of 2‐(Benzothiazol‐2‐ylthio)‐1‐phenylethanone and 2‐(Acetonylthio)Benzothiazole by C―S Bond Cleavage of 2‐(Acetonylthio)benzothiazole in KOH

New route for the synthesis of 2‐(benzothiazol‐2‐ylthio)‐1‐phenylethanone ( 6 ) and 2‐(acetonylthio)benzothiazole ( 1 ) by using phenacyl bromide and α‐chloroacetone, respectively, through carbon–sulfur bond cleavage reactions in a basic medium has been generated. Treatment of 1 with malononitrile and elemental sulfur afforded the corresponding derivative of 2‐amino‐3‐cyanothiophene ( 12 ), whereas treatment of 1 with cyanoacetohydrazide afforded the corresponding derivative of cyanoacetylhydrazone derivative ( 13 ). The structure of the synthesis compounds has been established on the basis of elemental analyses, ¹H‐NMR, ¹³C‐NMR, correlation spectroscopy, heteronuclear single quantum coherence, MS spectra, and X‐ray crystallographic investigations.