Theophylline Derivatives' In-vivo Analgesic and Anti-Inflammatory Activities

The reaction of theophylline and chloro-acetyl chloride produced an exceptional series of substituted theophylline derivatives (3A-3D), followed by ammonium thiocyanate and substituted aromatic aldehyde, and these synthesized derivatives were screened to study their analgesic and anti-inflammatory activities. UV, IR, H-1 NMR, mass spectral data, and CHN activities were used to describe the compounds, which were shown to be considerably efficacious at 100 mg/kg p.o., as well as experimental results that were statistically significant at the p <0.01 and p <0.05 levels.

Manipulating Interfacial Stability Via Absorption-Competition Mechanism for Long-Lifespan Zn Anode

The stability of Zn anode in various Zn-based energy storage devices is the key problem to be solved. Herein, aromatic aldehyde additives are selected to modulate the interface reactions between the Zn anode and electrolyte. Through comprehensively considering electrochemical measurements, DFT calculations and FEA simulations, novel mechanisms of one kind of aromatic aldehyde, veratraldehyde in inhibiting Zn dendrite/by-products can be obtained. This additive prefers to absorb on the Zn surface than H2O molecules and Zn2+, while competes with hydrogen evolution reaction and Zn plating/stripping process via redox reactions, thus preventing the decomposition of active H2O near the interface and uncontrollable Zn dendrite growth via a synactic absorption-competition mechanism. As a result, Zn–Zn symmetric cells with the veratraldehyde additive realize an excellent cycling life of 3200 h under 1 mA cm−2/1 mAh cm−2 and over 800 h even under 5 mA cm−2/5 mAh cm−2. Moreover, Zn–Ti and Zn–MnO2 cells with the veratraldehyde additive both obtain elevated performance than that with pure ZnSO4 electrolyte. Finally, two more aromatic aldehyde additives are chosen to prove their universality in stabilizing Zn anodes.

Synthesis, Characterization of Novel Schiff’s Bases of 2-(1H-tetrazol-5-yl) Pyridine and Evaluation of their Antitubercular Activity

This study aimed to prepare some new 2-(1H-tetrazol-5-yl) pyridine derivatives from Pyridine Nitrile as a starting materials and to evaluate the antitubercular activity against Mycobacterium Tuberculosis. The first step involves the reaction of 2-(1H-tetrazol-5-yl) pyridine with ethyl chloroacetate to form ethyl [5-(pyridin-2-yl)-1H-tetrazol-1-yl] acetate (A). In step II it was further treated with hydrazine hydrate to form 2-[5-(pyridin-2-yl)-1H-tetrazol-1-yl] acetohydrazide (B). The compound B was treated with different aromatic aldehyde to form N'-[(E)-substituted phenylmethylidene]-2-[5-(pyridin-2-yl)-1H-tetrazol-1-yl] acetohydrazide (Schiff Bases) (C1–C10). The compounds obtained were identified by spectral data. The antitubercular activity of synthesized compounds were evaluated against Mycobacterium Tuberculosis. The compound C4 and C10 was found to possess potent activity while compounds C2 and C3 shows moderate activity.

Improving the Solubility and Oral Bioavailability of a Novel Aromatic Aldehyde Antisickling Agent (PP10) for the Treatment of Sickle Cell Disease

Background: Aromatic aldehydes, with their ability to increase the oxygen affinity of sickle hemoglobin, have become important therapeutic agents for sickle cell disease (SCD). One such compound, voxelotor, was recently approved for SCD treatment. Methyl 6-((2-formyl-3-hydroxyphenoxy)methyl) picolinate (PP10) is another promising aromatic aldehyde, recently reported by our group. Like voxelotor, PP10 exhibits O2-dependent antisickling activity, but, unlike voxelotor, PP10 shows unique O2-independent antisickling effect. PP10, however, has limited solubility. This study therefore aimed to develop oral and parenteral formulations to improve PP10 solubility and bioavailability. Methods: Oral drug tablets with 2-hydroxypropyl beta cyclodextrin (HP-β-CD), polyvinylpyrrolidone, or Eudragit L100-55 PP10-binary system, and an intravenous (IV) formulation with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or HP-β-CD, were developed. The pharmacokinetic behavior of the formulations was studied in Sprague-Dawley rats. PP10, a methylester, and its acid metabolite were also studied in vitro with sickle whole blood to determine their effect on Hb modification, Hb oxygen affinity, and sickle red blood cell inhibition. Results: Aqueous solubility of PP10 was enhanced ~5 times with the HP-β-CD binary system, while the TPGS aqueous micelle formulation was superior, with a drug concentration of 0.502 ± 0.01 mg/mL and a particle size of 26 ± 3 nm. The oral tablets showed relative and absolute bioavailabilities of 173.4% and 106.34%, respectively. The acid form of PP10 appeared to dominate in vivo, although both PP10 forms demonstrated pharmacologic effect. Conclusion: Oral and IV formulations of PP10 were successfully developed using HP-β-CD binary system and TPGS aqueous micelles, respectively, resulting in significantly improved solubility and bioavailability.

Synthesis of Some Organic Hydrazine Compounds Using Microwave Radiation

This work was included the preparation of substituted organic hydrazine compounds from acid hydrazide (succinic dihydrazide and malonoicdihydrazide) through the reaction with different aromatic aldehyde compounds using microwave radiation. This study was also identified the product compounds by measuring its physical constants (melting point) and measuring infrared spectra. Confirmation for the structures of the prepared compounds by using infrared Spectro and measuring some physical constants, that sure the reactions were complete by using new energy radiation under green chemistry which accelerated the reaction in a few seconds and without byproduct. Keywords: Synthesis; Hydrazine; Characterization and microwave radiation

A NEWER METHODDEVELOPED FOR THE SYNTHESIS OF DIFERULOYL METHANE AND ITS DERIVATIVES

Here in the current research work we have developed newer method for the synthesis of diferuloyl methane(curcumin)Ca-q. MangnesiumHydroxide were found to be an effective and mild base for synthesis of curcumin and its derivatives obtained by reaction of one equivalent of acetyl acetone with two equivalent of corresponding aromatic aldehyde in microwave(240 W). The existingscheme offers severalaids such as high yield, less time, and environmentally friendly.

Recent Advances in Chemistry and Biological Activity of 2,6-Diphenyl piperidines

: The review discusses different methods for preparation of 2,6-diphenyl-piperidin-4-one derivatives. 2,6-Diphenyl-piperidin-4-one is prepared from aromatic aldehyde and acetone in ammonium acetate. Reaction of 1-phenylsulfinylpropan-2-one or 1-(4-chlorophenylsulfinyl)propan-2-one, aromatic aldehyde and ammonium acetate gives a series of 2,6-diaryl-2,3-dihydro-1H-pyridin-4-one 6a,b. 4-Phenyl-2-amino-1,3-butadienes reacts with N-allyl benzaldimine through Diels-Alder reaction to afford 2,6-diphenyl-4-piperidinone derivative 7. Also, reactions of 2,6-diphenyl-piperdin-4-one are discussed. The reactions of latter compounds can be on nitrogen atom or carbonyl function group or methylene group adjacent to carbonyl group. In addition, different applications of 2,6-diphenyl-piperidin-4-one are summarized.

Diastereoselective Synthesis of Spiro[carbazole-3,5'-pyrimidines] and Spiro[carbazole-3,1'-cyclohexanes] via Four-component Reaction

The functionalized spiro[carbazole-3,5'-pyrimidines] and spiro[carbazole-3,1'-cyclohexanes] were efficiently synthesized in satisfactory yields with high diastereoselectivity by CuSO4 catalyzed multicomponent reaction of indole-2-acetate, aromatic aldehyde and 1,3-dimethylbarbituric acid or dimedone. The reaction...