Phenylhydrazine Research Articles

Evaluation of haematinic activity of Kumara Veeriya Kaantha Chendhuram in phenyl hydrazine induced Anemia in experimental rats

Evaluation of haematinic activity of Kumara Veeriya Kaantha Chendhuram in phenyl hydrazine induced Anemia in experimental rats

Evaluation of haematinic activity of Kumara Veeriya Kaantha Chendhuram in phenyl hydrazine induced Anemia in experimental rats

The science of medicine is one of the fundamental requirements to well being of humans and their survival. Siddha system is one of the traditional systems of medicine. According to WHO, anaemia is one of the leading causes of death in worldwide. Anaemia is the most common blood disorder, affecting about one third of the global population. In classical Siddha literature, Kumara Veeriya Kaantha Chendhuram is one of the formulation mentioned in Anupoga Vaithiya Navaneetham – part I helps in overcoming iron deficiency anaemia. The ingredients of the formulation include Kaantham (magnetic oxide of iron) and Thara (Mollugo oppositifolia).The present study aims to evaluate haematinic activity by Phenyl hydrazine induced anaemia in animal models. The evaluation was carried out in Wistar albino rats. The effect of standard drug was comparable to those of the test drug. The blood parameters in animals treated with the test drug exhibited a highly statistical significant elevation when compared to control group.

Online column preconcentration for speciation and selective determination of Cr(III) in natural water samples using flow injection with chemiluminescence detection.

A simple, rapid, sensitive and inexpensive approach is described in this work based on a combination of solid-phase extraction of 8-hydroxyquinoline (8HQ), for speciation and preconcentration of Cr(III) and Cr(VI) in river water, and the direct determination of these species using a flow injection system with chemiluminescence detection (FI-CL) and a 4-diethylamino phenyl hydrazine (DEAPH)-hydrogen peroxide system. At different pH, the two forms of chromium [Cr(III) and Cr(VI)] have different exchange capacities for 8HQ, therefore two columns were constructed; the pH of column 1 was adjusted to pH3 for retaining Cr(III) and column 2 was adjusted to pH1 for retaining of Cr(VI). The sorbed Cr(III) and Cr(VI) species were eluted from columns using 3.0ml of 0.1N of HCl and 3.0ml of 0.1N of NaOH, respectively. The flow injection-chemiluminescence (FI-CL) method is based on light emitted due to the oxidation of DEAPH by the H2 O2 in the presence of Cr(III), which catalyzes the reaction. The flow cell is a transparent coiled tube made from glass (2.0×4.0, inner and outer diameter) and located close to the photodetector. The flow parameters: flow rate, sample volume, flow cell length, and distance to the CL detector were studied and optimized. Under optimum flow conditions, the Cr(III) concentration can be determined over the range 5-350 μg L-1 with a limit of detection of 1.2μg L-1 , as the Cr(III) concentration is proportional to the intensity of the CL signal. The relative standard deviations (%) for 10 and 50 μg L-1 Cr(III) were 1.2% and 3.2%, respectively. The effects of Al(III), Cd(II), Zn(II), Hg(II), Pb(II), Co(II), Cu(II), Ni(II), Mn(II), Ca(II), and Fe(III) were investigated. The proposed method is highly selective and sensitive, enabling a rapid determination of the Cr(III) amount in the presence of other interfering metals. Finally, the FI-CL method was examined in five river water samples with excellent recoveries.

Ring transformation reactions of 4-hydroxy-3-nitro-6-phenyl-6H-pyrano[3,2-c]quinoline-2,5-dione and antioxidant activity

4-Hydroxy-3-nitro-6-phenyl-6H-pyrano[3,2-c]quinoline-2,5-dione was reacted with some 1,2-binucleophiles, such as hydrazine, phenylhydrazine, and hydroxylamine hydrochloride affording the interesting pyrazolyl and isoxazolylquinolinones. Nucleophilic reactions of 3-nitropyranoquinolinone with different 1,4-binucleophiles, leading to a variety of novel diazepinyl, oxazepinyl, and thiadiazepinylquinolinone derivatives, were described. The structure of compounds was proved by elemental analysis and spectral data. Selected products were screened for their antioxidant activity and showed higher radical scavenging abilities.

Synthesis and Characterization of New Pyrazoline and Isoxazoline Derivatives Based on Fluorene

The aim of the present work is a synthesis of new fluorene derivatives containing heterocyclic moieties. These compounds were synthesized in four groups, each group containing five compounds. The first group was made up of 2-(3-aryl-2-propenoyl) fluorene derivatives (1a-e) synthesized from the reaction of 2-acetyl fluorene with appropriate aromatic aldehyde in the presence of sodium hydroxide. The other three groups involved compounds produced from the reaction of (1a-e) with hydrazine hydrate (99%) in presence of acetic acid (96%) to give 1-acetyl-5-aryl-3-(fluoren-2-yl) pyrazoline derivatives (2a-e), and with phenyl hydrazine in presence of piperidine to produce 1-phenyl-5-aryl-3-(fluoren-2-yl) pyrazoline derivatives (3a-e), and with hydroxylamine hydrochloride in presence of pyridine to obtain the 5-aryl-3-(fluoren-2-yl) oxazoline derivatives (4a-e). All the compounds of the above three groups were substituted at position (5) in pyrazoline and isoxazoline ring with different aryl groups according to aromatic aldehyde used in the preparation of the first group series compounds. The synthesized compounds were identified by spectroscopic methods: FT-IR and 1H-NMR

Antiviral effects of the fused tricyclic derivatives of indoline and imidazolidinone on ZIKV infection and RdRp activities of ZIKV and DENV

The prevalence and ravages of Zika virus (ZIKV) seriously endanger human health, especially causing significant neurological defects in both neonates as pediatric microcephaly and adults as Guillain–Barré syndrome. In this work, we studied anti-ZIKV effects of the fused tricyclic derivatives of indoline and imidazolidinone and discovered that some of them are valuable leads for drug discovery of anti-ZIKV agents. The current results show that certain compounds are broad-spectrum inhibitors of ZIKV- and dengue virus (DENV)-infection while distinctive compounds are selective ZIKV inhibitors or selective DENV inhibitors. Compounds of 12, 17 and 28 are more active against Asian ZIKV SZ-VIV01 strain than African ZIKV MR766 strain. It is valued that silylation makes six TBS compounds of 4-nitrophenyl hydrazine series and phenyl hydrazine series more active against ZIKV infection than their phenols. Time-of-addition and withdrawal studies indicate that compound 12 majorly acts on post-infection of RNA synthesis stage of ZIKV life cycle. Moreover, compounds of 12, 17 and 18 are anti-ZIKV agents with the inhibitory activities to ZIKV NS5 RdRp while 12 doesn't inhibit DENV infection even though it is a DENV RdRp inhibitor, 17 is an active agent against DENV infection but is only a weak DENV NS5 RdRp inhibitor, and 28 is inactive against DENV infection and not a DENV NS5 RdRp inhibitor. As a result, a compound's antiviral difference between ZIKV and DENV is not always related to anti-RdRp difference between ZIKV RdRp and DENV RdRp, and structural features of a compound play important roles in executing antiviral and anti-RdRp functions. Further discovery of highly potent broad-spectrum or selective agents against infection by ZIKV and DENV will be facilitated.

Development of New Method for the Synthesis of Pyrazole Derivative

The pyrazole ring is a well-known structural originate in numerous pharmaceutically active compounds. Pyrazole framework plays a vital role in biologically active compounds and therefore represents an appealing pattern in medicinal chemistry [1-2]. likewise, pyrazole derivatives have showed important biological activities, such as anti-microbial [3], analgesic [4], anti-inflammatory [5] and anticancer [6] activities. This gave a great momentum to the search for probable pharmacologically active drugs carrying pyrazole substituents. In persistence of former work on the development of the suitable synthetic method for biologically active molecules [7–10] using some of the green pathway and considering the above urgent need here it was thought worthwhile to develop better synthetic protocol by carrying the cyclocondensation of multicomponents, aromatic aldehydes, ethylacetoacetate and phenyl hydrazine under neat condition or in organic medium.

New Dual Inhibitors of SARS-CoV-2 Based on Metal Complexes with Schiff-Base 4-Chloro-3-Methyl Phenyl Hydrazine: Synthesis, DFT, Antibacterial Properties and Molecular Docking Studies

This paper explores a dual inhibition of main protease (Mpro) and nonstructural protein 10/nonstructural protein 16 (NSP16) methyltransferase complex as the key targets for COVID-19 therapy. These are based on the new Schiff-base ligand that was obtained from the condensation of (4-chloro-3-methyl phenyl) hydrazine with 2-pyridine-carboxaldehyde and its novel Schiff-base metal complexes. These include Ni(II), Pd(II), Pt(II), Zn(II), and Hg(II). The newly synthesized compounds have been characterized using FT-IR, 1H NMR, 13C NMR, and elemental analysis. The results suggested that the Schiff-base ligand is coordinated as a bidentate ligand through the nitrogen atoms of the azomethine group and pyridyl ring. In addition, the biological activity of the prepared complexes was examined against Pseudomonas aeruginosa and Staphylococcus aureus, and the results showed that the Zn(II) complex has the highest activity compared with other compounds. The active sites were found by looking at the molecular electrostatic potential (MEP) maps of the above ligands and complexes. The activity of the compound and its Ni(II) and Zn(II) complexes against Mpro and NSP10/ NSP16 was investigated using a molecular docking approach. They showed excellent binding energies ranging from −5.9 to −7.2 kcal/mol and −5.8 to −7.2 for Mpro and NSP16, respectively. All conformers of the metal complexes were docked with the active site of the NSP16 receptor, showing a binding affinity of 100%. According to our knowledge, this was the first report of these metal complexes as dual inhibitors for Mpro and NSP16 of SARS-CoV-2.

Haematic Potentials of Rhynchospore Corymbosa and Olax Subscorpioïdea Extract in Phenylhydrazine – induced Anaemic Rats

The decoction of the whole plant of Rhynchospora corymbosa and Olax subscorpioïdea leaves are used by the Local traditional healers in the department of Korhogo (Northern Côte d’Ivoire) to treat patients with sickle cell disease. This study was designed to assess, the antianemic potential of these plants extract. Anemia was induced with phenylhydrazine hydrochloride in rats. Animals were divided in normal (N), control (C), test (T), and reference (R) groups. T group included ill-induced Animals treated with R. corymbosa and O. subscorpioidea extracts, and R group ill-induced animals treated with vitamin B9 for anemic animals. Dosing was made as 1-day single dose repeated dose. In anemic animals, the production rate of RBC was significantly (p < 0.001) higher in T group as compared to C group. R. corymbosa whole plant and O. subscorpioidea leaves extracts have a haematic potential. The anti-anaemic effect may partly explain their use in patients with sickle cell disease who are affected by a deficiency of erythrocytes and its components.

Four Component One Pot Synthesis of Benzyl Pyrazolyl Coumarin Derivatives Catalyzed by Metal-Free, Heterogeneous Chitosan Supported Ionic Liquid Carbon Nanotubes

In this present communication, four component, one pot synthesis of benzyl pyrazolyl coumarin (5a-m) derivatives achieved from the condensation of phenyl hydrazine (1), ethyl acetoacetate (EAA, 2), various substituted benzaldehyde (3), and 4-hydroxy coumarin (4) in EtOH/H2O using metal-free chitosan supported ionic liquid carbon nanotubes (CSIL@CNTs, 10 mol%) as heterogeneous catalyst reflux at 50 °C for 25–30 min. The optimized conditions and excellent yields of the products were reported. All the synthesized compounds were charecterized by the spectroscopic methods. The main advantages of this reported method using CSIL@CNTs. leads to effective conversions were achieved under reflux conditions without the need of an inert atmosphere. In adition, shorter reaction time, simple work up procedure, easy preparation of the catalyst, and chemoselectivity were siginificantly recorded.

Terminalia catappa attenuates phenylhydrazine-induced anaemia and hepato-renal toxicity in male Wistar rat by boosting blood cells, modulation of lipoproteins and up-regulation of in vivo antioxidant armouries

Aim This study investigated the haematinic, antihyperlipidaemic, hepato-renal protective effects of Terminalia catappa aqueous leaf extract on male Wistar rats exposed to phenylhydrazine toxicity. Methods Animals were exposed to phenylhydrazine (PHZ) 50 mg/kg intraperitoneal for two consecutive days thereafter, treated with T. catappa extract (100 mg/kg and 200 mg/kg) orally for 21 days. After the experimentation, animals were sedated with ketamine (70 mg/kg) and euthanized by cervical dislodgement. Blood and organs were collected for haematology and biochemical studies following standard laboratory methods. Results Our study showed that T. catappa significantly increased erythrocytes, haemoglobin, haematocrit and high density lipoprotein as well as down-regulating leukocytes, thrombocytes, ALP AST, ALT creatinine, urea, total cholesterol as well as low density lipoprotein. The liver, kidney and spleen antioxidant defence were also up-regulated against the adverse effect caused by phenylhydrazine exposure. Conclusion Terminalia catappa attenuated Phenylhydrazine-induced anaemia and hepato-renal toxicity in male Wistar rat by boosting blood cells, modulation of lipoproteins and up-regulation of in vivo antioxidant armouries.

Phytochemical and Anti-Anemic Properties of the Aqueous Extract of Pseudarthria hookeri (Fabaceae) Leaves

In order to contribute to the valorization of plants used in African traditional medicine for the improvement of the health of the populations, we undertook this study to evaluate the therapeutic effectiveness of an aqueous extract of leaves of Pseudarthria hookeri (Fabaceae), a plant reputed to be anti-anemic. Qualitative phytochemical tests performed with the aqueous extract of Pseudarthria hookeri (Fabaceae) leaves revealed the presence of sterols, polyterpenes, polyphenols, catechic tannins, flavonoids, alkaloids, quinones and saponosides. The acute toxicity study of the aqueous extract of Pseudarthria hookeri leaves in female mice gave an estimate, according to the OECD-423 guidelines, of the 50% lethal dose (LD50). The results show that the administration of aqueous extract of Pseudarthria hookeri leaves at a dose of 2000 mg/kg bw and then at a dose of 5000 mg/kg bw did not induce any mortality in these animals during 14 days of observation; this allows us to conclude that aqueous extract of Pseudarthria hookeri leaves is not toxic by the oral route. Anemia was induced by administration of phenylhydrazine hydrochloride (4 mg/kg bw) for 6 days. Oral administration of aqueous extract of Pseudarthria hookeri leaves at doses of 50, 200, 1000 and 2000 mg/kg bw and the reference treatment (Ranferia hookeri) for 6 days did not induce anaemia. and the reference treatment (Ranferon®) resulted in normalization of red blood cell count, haemoglobin concentration, haematocrit, mean corpuscular haemoglobin volume (MCV), mean corpuscular haemoglobin concentration (MCHC) and Mean corpuscular haemoglobin level (MCHL) in anaemic rats compared to the white control rats. In conclusion, this study showed that Pseudarthria hookeri leaves have similar properties to Ranferon® in rats, which justifies the traditional use of this plant in the treatment of anaemia.

Effect of wheat germ oil on phenylhydrazine-induced toxicity in male albino rats

Wheat germ oil (WGO) is a natural source of antioxidant such as glucosylated hydroquinones, tocopherols and it is an excellent source of polyunsaturated fatty acids. The point of the present study is to see how efficient is the WGO against phenylhydrazine (PHZ) induced hemotoxicity in rats. Rats were divided into five groups (six rats each); control group (normal rats), WGO group (administrated by daily oral dose of WGO, 300 mg/kg b.w.), PHZ group (injected intraperitoneally with a daily dose of PHZ, 60 mg/kg b.w. for 3 consecutive days), treated group (injected with PHZ then after 3 days administered by WGO) and protective group (administrated daily by WGO for 11 days then injected with PHZ). The experimental trial was continued for a total period of 14 days. The results showed that the PHZ induced significant decreases in hematological parameters (RBCs, Hb, Hct, PLT), serum proteins (total protein, albumin and globulin) and antioxidant enzymes (CAT, GPX and SOD) activity and significant increases in white blood cells (WBCs), erythropoietin hormone, serum ferritin level, serum liver function parameters (ALT, AST, TBIL and ALP), serum kidney function parameters (creatinine, urea and uric acid) and malondialdehyde (MDA) content. Administration of WGO improved the hematological parameters, erythropoietin hormone, ferritin level, serum proteins, liver function enzymes, kidney function parameters, antioxidant enzyme activities and MDA content in rats injected with PHZ. In conclusion, the results of the present study revealed that the WGO has a therapeutic and protective roles in improving the hemolytic anemia and toxicity induced by PHZ.

Possible role of pomegranate fruit in reversing renal damage in rats exposed to Phenylhydrazine.

Pomegranate granatum (molasses and peels) and its constituents showed protective effects against natural toxins such as phenylhydrazine (PHZ) as well as chemical toxicants such as arsenic, diazinon, and carbon tetrachloride. The current study aimed to assess the effect of pomegranate molasses (PM), white peel extract, and red peel extract on nephrotoxicity induced by PHZ. 80 male rats were divided into eight equal groups; a control group, PM pure group, white peel pomegranate pure group, red peel pomegranate pure group, PHZ group, PM + PHZ group, white peel pomegranate + PHZ group and red peel pomegranate + PHZ group. Kidney function, inflammation markers, antioxidant activities, and renal tissue histopathology were investigated. The results revealed that PHZ group showed a significant increase in lactate Dehydrogenase (LDH), malondialdehyde (MDA), creatinine, uric acid, BUNBUN, C - reactive protein (CRP), tumor necrosis factor, thiobarbituric acid reactive substances (TBARSs), and total antioxidant capacity (TAC) with a significant decrease of catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD) as compared with a control group. Other pomegranate-treated and PHZ co-treated groups with pomegranate showed a significant decrease of LDH, MDA, creatinine, uric acid, BUN, tumor necrosis factor, TBARSs, and TAC with a significant increase of CAT, GPx, and SOD as compared with PHZ group. Collectively, our data suggest that red, white peels, and molasses have anti-toxic and anti-inflammatory effects on renal function and tissues.

Direct amidation of acids in a screw reactor for the continuous flow synthesis of amides.

A simple and efficient solvent-free protocol for continuous flow synthesis of amides at room temperature is developed using easily available starting materials. N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC.HCl) was used as the reagent for the formation of an amide bond without using any metal catalyst or additives. A jacketed screw reactor when operated over a residence time of 30 300 s helped achieve almost complete conversion. This approach is extended for the synthesis of 36 derivatives and 2 bioactive molecules using different substrates having different aliphatic mono and di-acids as well as aromatic acids, including aromatic hetero-acid compounds and phenyl hydrazine. The target amide was scaled up to 100 g with an average 90% yield.

Synthesis of novel pyrazolic analogues of chalcones as potential antibacterial and antifungal agents

The present includes the synthesis of pyrazoline derivatives using chalcones and phenyl hydrazine in the presence of ethanol. It also reveals that 2-pyrazoline complexes are physiologically active and may be used in a variety of therapeutic functions. FT-IR, 1H-NMR, 13C-NMR, LC-MS, and elemental analyses were used to characterise newly synthesised phenyl-pyrazoline derivatives. The antimicrobial activity of the synthesised compounds was assessed using the agar well diffusion assay and the Minimum Inhibition Concentration (MIC). Compounds 4b, 4f, and 4h have exhibited remarkable antibiotic action against bacterial strains such as Staphylococcus aureus, Bacillus subtilis, Salmonella. Typhi, and Shigella sp. On the other hand, compound 4h had significant antifungal activity against Candida albicans and Aspergillus fusarium and was a highly promising agent when compared to standard nystatin.

Fischer indole synthesis in DMSO/AcOH/H2O under continuous flow conditions

A new continuous flow synthetic method for preparing indole and its derivatives are successfully developed to overcome the disadvantages of traditional batch methods, such as low conversion rates, long reaction times, and amplification effects. The method represents a sustainable and efficient preparation of indole and its derivatives without the need for additional catalysts. By investigating the effects of the reaction temperature, the solvent, the equivalence ratio, and the residence time, high conversion rates and excellent yields were simultaneously achieved within 20 min under optimized conditions. For the template reaction, DMSO/H2O/AcOH = 2:1:1 is used as the solvent, the reaction temperature is 110 °C, and the ratio of phenylhydrazine hydrochloride to cyclopentanone is 1:1.05. Indole and a wide array of its derivatives are synthesized to verify the universality of the method, and most of the reactions exhibit satisfactory conversion rates and high yields are obtained. This new continuous flow method is more suitable for industrial scale-up relative to traditional batch methods.

Visible light-induced direct and highly selective C–H functionalization of quinoxalin-2(1H)-one without orientating group

Using eosin Y and KI as photocatalysts to facilitate the conversion of quinoxaline-2(1H)-one and phenylhydrazine hydrochloride compounds into corresponding 3-arylated quinoxaline-2(1H)-one, a simple and efficient synthesis method has been developed.

Determination of Diclofenac Sodium in Pharmaceutical Preparations by Computational Image Scanning Densitometry

Diclofenac sodium is a nonsteroidal anti-inflammatory drug which cures by reducing substances in the body that cause pain and inflammation. There is always a risk of heart attack and stroke in case of taking excess of the drug. In present study a simple, fast and cost-effective method is devised for the assay of diclofenac sodium in locally available pharmaceutical preparations. The method is based on the reaction of the drug with 2, 4-DNPH (2, 4-Dinitro phenyl hydrazine). Micro-quantities of the drug gave green coloured spots when mixed with 2,4-DNPH on a pre-coated TLC plate, in the presence of potassium iodate and lithium hydroxide. The spots were scanned by using a flatbed scanner and the images obtained were computationally quantified with the help of custom-made software to measure the optical density. The reaction parameters were optimized, and the results were compared with the standard spectrophotometric method

Synthesis of Ketamine Derivatives by Mannich Reactions

Arylcyclohexylamine Ketamine (HCL) has played an important role in Veterinary and Human Medicine as safe and reliable anesthetic agent but asit produces dysphoria several new derivatives of Ketamine have been synthesized till date. In this Research we have Utilized Mannich reaction to Synthesize The ammonia, primary amine and secondary amine are treated with hydrochloric acid and then added to the formaldehyde. Three novel derivatives were synthesized namely2-(2-chlorophenyl)- 6-[(diethyl amino) methyl]-2-(methylamino) cyclohexanone by RXN:102 Mannich Reaction of Ketamine with Di-ethylamine , rxn 113 2-(2chlorophenyl-6-dinitrophenyl hydrazine-methyl2(methylamino) cyclohexanone by Reaction of Ketamine with Di-nitro Phenyl Hydrazine & Rxn: 601. Mannich Reaction of Ketamine with Piperazine to form (2-chlorophenyl)-2-(methylamino)-6-(piperazine -1-yl) methyl cyclohexanone. Other reactions were also undergone to prepare oxazolidine derivatives of ketamine namely Synthesis of ketamine dioxolane derivative:Ketal and Hemiaminal Formation , Rxn: 103 Reaction of Ketamine with Glycerin [6-(2-chlorophenyl)-6-(methylamino)-1, 4-dioxaspiro [4.5] dec-2-yl] methanol and Rxn: 801 Reaction of Ketamine with Ephedrine N ,3,4-trimethyl-2,6 diphenyl-1oxa-4azaspiro [4.5] decan-6-amine derivative was formed. Thin layer chromatography of the synthesized derivatives was performed by using a solvent system of ethyl acetate and chloroform (50:50) and the RF values were calculated. The solubility test proves that compounds obtained from ketamine are polar in nature. All derivatives show similarity in solubility of ketamine. Although the melting points were not exactly comparable to that of ketamine, the range was not more than 5-10°C. This relatively narrow range of melting points proved that these were pure compounds. NMR spectroscopy was performed on all newly synthesized derivatives of ketamine. The notable ones obtained from reactions i.e. Rxn 102, 113, 103, 601and 801. The results of spectroscopy demonstrate that the compounds obtained were completely new species however they were structurally related to ketamine. These derivatives synthesized and confirmed by NMR technology. The derivatives can potentially be formulated for therapeutical purpose. Despite some limitations which are being considered in current drug design, the derivatives have the potential to develop into chemically modified entities that can play a major role in clinical therapeutics. Additional research studies will potentially help to determine the advanced method for high and sophisticated yield of these derivatives. Moreover, synthesis of ketamine metabolites namely N-demethyl compound and N-demethyl-5,6-dehydro analogues is established. However, further studies and modifications of these compounds will open new ventures of drug design and development of clinical implications in health care system.