Derpharmachemica

The aim of this study was to investigate the anthelmintic activity of leaves of Amaranthus dubius, Basella alba and Cleome gynandra against adult Indian earthworm Eisenia fetida. E. fetida was selected as a model for anthelmintic activity due to its anatomical and physiologicalresemblance with the intestinal round worm parasites of human beings. Normal saline was used as the control while Albendazole drug at 25 mg/ml and 50 mg/ml were used as the standard drug. Three concentrations of leaves extract (100 mg/ml, 200 mg/ml and 300 mg/ml) of A. dubius, B. alba and C. gynandra were used to study the Anthelmintic activity. The 300 mg/ml proved to be very active by paralyzing and killing the earthworms in a shorter time. At 300 mg/ml A. dubius showed 18 min for paralysis stage and 28 min for death stage of E. fetida. Synergistic studies of the plants against Helminths were also carried out where two plants were combined and all had the same concentration (200 mg/ml). B. alba and A. dubius c...

A direct and efficient approach for the preparation of 1H-pyrazolo[1,2-b]phthalazine-5,10-diones has been developed through one pot fourcomponent reaction of easily available phthalic anhydride, hydrazine monohydrate, aromatic aldehyde and malononitrile or ethyl acetoacetate catalyzed by nano particulate NiFe2O4 , a heterogeneous base catalyst at 55oC. This protocol offers excellent yield of products within short reaction time, easy work up, easy to separate and recyclable catalyst.

Exposure to Alternariol or Patulin toxin is known to have toxic effects in different animal species, and to express toxicity in cells. Purpose: The aim of this study is to compare the protective effect of Neem and Propolis extracts in hepatorenal toxicity caused by somemycotoxins. Study design: Animals were divided into seven groups each of 5 animals and received single oral dose of 3 ml/rat, group 1, received A. alternata toxin; group 2, Alternaria alternate plus neem extract; group 3, A. alternata plus propolis extract; group 4, received Penicillium expansum toxin; group 5, P. expansum Patulin extract plus neem extract; group 6 P. expansum Patulin extract plus propolis extract; group 7, received normal water as a control. Methods: ALT, Urea and Creatinine were detected in all groups after two weeks of feeding, the expression of Caspase-3 and iNOS in liver and kidney tissues were assessed immunomorphometrically by image analysis system. Results: Animals received Alternariol or Patul...

In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. Theimplication of different members of Histone Acetyl Transferase (HAT) in cancer disease is well documented in literature, however the clinicallyeffective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided auseful start point to develop HAT inhibitors. Consequently, preparation and biological evaluation of a focused library of 4-aryl-2- hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5ab), (6a-b) studied by either conventional method and free solvent microwave one pot method, the activity against different cancer cell-lines and the antimicrobial activities against different organisms also studied. It was found that all of the prepared thaizoles derivatives were active toward many c...

4-oxo-5-(3,4,5-trimethoxy-benzylidene)-4,5-dihydrothiazol-2-yl)-acetonitrile 1 was prepared and treatment with sodium azide, phenylisothiocyanate, 5-bromosalicylaldehyde, thioacetamide and ethylacetate to give the corresponding 2-substitute-4-oxo-5-(3,4,5-Trimethoxybenzylidene-4,5-dihydrothiazole-2-yl) derivatives 2,3,5,6 and 8. Treatment of 3 and 6 with phenacylbromide gave 4 and 7a also 4-oxo-2-[4-oxo5-(3,4,5-trimethoxy benzylidene)-4,5-dihydro-thiazol-2-yl)-butyronitrile 8 when reacted with malononitrile, 2-cyanoacetohydrazide, hydrazine hydrate, benzaldehyde and 2-amino-2-(hydroxylmethyl) propane-1,3-diol afforded 9,13,15, 16 and 17. Treatment of compound 9 with sulfur gave 10 which in turn treated with p-nitrobenzaldehyde to give Schiff base 11, which on further treatment with thioglycollic acid gave 12. Cyclization of compound 13 with acetic acid gave 14. The newly synthesized compounds screened for their in vitro antitumor activity against human cancer cell line.

This article describes the biological activities of essential oils of three species of Satureja. The choice of plants and activities studied was motivated by the frequent traditional use of Satureja abriquetti, Satureja atlantica and Satureja alpina by indigenous populations for the efficacy and virtues they discovered. The aim of the experiments is to prove the antioxidant, anti-inflammatory and antinociceptive activities of theessential oils of S. briquetti, S. atlantica and S. alpina. The antioxidant activity was evaluated by three different methods namely the free radical scavenging, the Ferric Reducing Antioxidant Power and the phosphomolybdenum method. The Carrageenan induced paw oedema in rats assay was used to evaluate the anti-inflammatory activity of essential oils. In order to prove the antinociceptive activity, the plantar model was chosen. The three essential oils have interesting antioxidant powers, especially by the reductive and phosphomolybdenum methods where the act...

Riociguat is a potent, oral stimulator of soluble guanylate cyclase for the treatment of pulmonary hypertension, is prepared via an efficient, noninfringing synthesis route from commercially available diethyl malonate via [N-Methyl(benzyl)amino]propanedinitrile.

The development and validation of a simple, rapid, precise and accurate RP-HPLC has been described for the simultaneous assessment and invitro dissolution of Olmesartan (OLM), Amlodipine (AML) and Hydrochlorothiazide (HCTZ) in their combined dosage forms. Separation was performed on Inertsil ODS-3 column (C18, 150 mm x 4.6 mm, 5 μm) using photodiode array (PDA) detection at 255 nm. The mobile phaseconsisted of phosphate buffer (pH 3.5) and acetonitrile, in a gradient program (time in minutes/acetonitrile %: 0.00/30, 1.00/30, 8.30/70 and9.00/30) at a 1.3 ml min-1flow rate. Analytes were perfectly resolved with retention times of 2.59, 4.99 and 7.48 min for OLM, AML, and HCTZ,respectively. Following the recommended procedure, linear calibration graphs extended for 0.20-28.00, 0.05-7.00 and 0.12-17.50 µg ml -1 with detection limits of 0.021, 0.002 and 0.012 µg m; -1 and quantitation limits of 0.063, 0.036 and 0.007 µg ml -1 for the assay and in-vitro drug release of OLM, AML and HCTZ, ...

Compounds which are having an isoindole moiety are important classes of the bioactive molecules. Several isoindoles and their fused derivatives were synthesized and evaluated for their efficiency as antimicrobial agents in the past years. However, several novel problemsappeared with the treatment of various infections (resistant bacterial or nosocomial infections, multidrug-resistant bacterial, rare andaggressive infections), thus medicinal or pharmaceutical chemists are challenged to discover and find improved novel and more efficient drugs. The aim of this overview is to summarize the most efficient and promising isoindole derivatives to promote these developments of potent and safe drugs with fewer side effects.

The present study involves the development of certain thiazolo[3,2-a]pyrimidin-5-ones linked through an ethylene bridge to various amines. Thenewly synthesized compounds 4-6(a-c) were subjected to in vitro anticancer evaluation using NCI antitumor screening. The target compounds showed observed activity against Renal UO-31 cancer cell line with cell growth promotion 52.72%-64.52%. Assessment of toxicities, druglikeness, and drug score profiles are reported. Some of the synthesized compounds showed good docking scores with potential anticancer targets. In vitro anticancer evaluation, together with in silico studies, revealed that compounds 5c, 4a, and 4b could be considered as promising leads for further development of more potent anticancer agents.

(z)-4-((4-amino-[1,1’biphenyl]-4-yl)amino)pent-3-en-2-one,L3c1(z)-5-((4’-amino-[1,1’biphenyl]-4-yl)amino)hept-4-en-3-one L3d1, (z)-3-((4’- amino-[1,1’biphenyl]-4-yl) amino)-1-phenylbut-2-en-1-one L3e1, were synthesized from the condensation of acyclic -1,3- betadiketone derivatives and Benzidine using ethanol. The presence of a linkage of two phenyl groups in the para position in relation to the amine groupmakes this particular class of enaminones have prospective added advantages and hence functionalization. The advantages offered by this method presented are use of mild, cheap, shorter reaction time for complete enamination and an aspect of green Chemistry. 

Due to metabolic stress secondary to hyperglycemia and safety issues of primary pharmacologic agents used for the treatment of diabetes, safer plant-based natural products are being evaluated as alternative supplements in ensuring normal basal glucose level both in normal and diabetic patients. Recent studies have focused on developing such herbal drugs from plants like Syzygium cumini. This plant is readily used as an herbal drug in the Philippines due to its known medicinal properties; there are no sufficient studies currently available in the literature that validates the efficacy of the local duhat variety against hyperglycemia especially that of the leaf extract. In this study, crude methanolic extract of S. cumini leaves was evaluated for its anti-hyperglycemic property. Upon administration of treatment in glucose challenged hyperglycemic mice at 0, 0.5, 1.0, 1.5, and 2.0 h, results showed that the mean blood glucose levels of hyperglycemic mice treated with glibenclamide had a ...

A series of halogenated Semicarbazones (SCs) and Thiosemicarbazones (TSCs) (11-30) were synthesized from mono fluorinated-, bromine- and chlorinated acetophenones (1-10). Structures were confirmed by Nuclear Magnetic Resonance (NMR) spectral data. Both effects, thehalogenated substituent and the position of the substitution on the antiproliferative activity, were systematically investigated for the first time.Cytotoxic activity was evaluated, using tetrazolium salt method (MTT), in two murine cell lines: CT26 (colon cancer) and B16 (melanoma). Only, o-, m- and p-fluorinated SCs and TSCs showed significant cytotoxic activity. Among them, compounds with fluorine at m-position in the phenyl ring showed the superior antiproliferative activity. The most actives derivatives were: m-Fluoroacetophenone semicarbazone (13) (µM; IC50 =7.2 ± 0.5, IC50=8.1 ± 0.2) and m-Fluoroacetophenone Thiosemicarbazone (23) (µM; IC50 = 3.1 ± 0.4, IC50=4.9 ± 0.5) in CT26 and B16, respectively. In addition, stu...

This work describes anticancer and antioxidant biological testing for new derived compounds form cycloheptathienopyrimidine nucleus along with their synthetic approach. The anticancer activity was tested against cancerous human breast cells MCF-7 and human liver cancer cell lineHEPG-2 in reference to Doxorubicin. All the tested products showed significant cytotoxic activity. Six out of twelve tested compounds showed anticancer activity even more than that of reference standard Doxorubicin against MCF-7 cell line whereas, eight compounds declared cytotoxic effect more than the reference standard against cell line HEPG-2 reflected by their IC50S. Furthermore, six of the top ranked anticancer results were tested for their antioxidant effect with DPPH method in reference to Ascorbic acid, three of which gave 100% free radical scavenging activity

The physico-chemical properties of the biodiesel prepared from Sweet almond seed oil was determined and discussed in accordance with ASTM D6751 and DIN 14214 standards for biodiesel. The influence of the fatty acid composition and functional groups on the fuel related propertieswas carried out using Gas Chromatography-Mass Spectrometry (GC-MS) technique and Fourier Transform Infrared Radiation (FTIR)spectroscopy analyses respectively. The presence of C-H indicates the presence of properties as pour and cloud point that affect the performance of biodiesel during cold weather engine operations but the biodiesel sample was found to contain more C=C that can cause it to remain in liquid state with tendency of poor storage stability. It was equally observed that the Sweet Almond Seed Oil Methyl Ester (SASOME) is mainly composed of monounsaturated fatty acid and expected to possess low values for density, viscosity, heating value and thermal efficiency with average cetane number. This woul...

Active pharmaceutical ingredient, 2-Cyclohexylcarbonyl-4-oxo-1,2,3,6,7,11 b- hexahydro-4H-pyrazino[2,1-a] isoquinoline has been achievedby deep eutectic solvent (DES) which is an efficient, green and novel route of synthesis. This drug is used in treatment of Schistosomiasis. The Nalkylation reactions with inexpensive raw materials proceed efficiently with improved yield that makes synthesis cost effective. The present reaction offers excellent selectivity which lacks product of N, N-dialkylation. Ease of recovery and reusability of DES makes this process efficient and environment friendly. 

A touchy and precise excessive-overall performance liquid chromatography combined with triple quadrupole mass spectrometry (lc-ms/ms) method, working in the positive ionization mode, for quantifying of Amlodipine in human plasma using Amlodipine maleate d4 as inner widespread (IS) was advanced and confirmed. The analyte and internal standard were extracted by using solid-section extraction with a aggregate of 5 mm ammonium acetate in 0.1% formic acid: methanol: acetonitrile (40: 30: 30%). The Chromatographic separation was performed on zorbax sb, c18, 50* 4.6 mm, 3.5 mm. The analytical approach is legitimate for the estimation of amlodipine, in human plasma over a number 0.100 ng/ml to 9.990 ng/ml with the detection of amlodipine m/z-409.10 (determine) and 238.00 (product) and internal standard amlodipine maleate d4 m/z-413.20 (determine) and 238.00 (product) in positive ion mode. The results of carryover test, matrix impact, linearity, precision and accuracy, stabilities, dilution ...

Distribution studies of Benzoic acid were done by taking solvents like Benzene, toluene, xylene, n-hexane, cyclohexane, chloroform, carbon tertrachloride, isobutyl alcohol and isoamyl alcohol. For this 10-3dm3benzoic acid in aqueous phase was distributed in these solvents andconcentration of benzoic acid was found out by titration against 0.1 N NaOH. This distribution ratio was calculated and the effect of several physical parameters on distribution of Benzoic acid was analysed.