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Malaria is a life threatening disease caused by microscopic parasites called Plasmodium that are transmitted to human beings by mosquitoes. Single celled Eukaryotic plasmodium parasite is responsible to cause malaria in human beings and is transmitted by bite of Anopheles species mosquitoes. Resurgence of malaria towards the end of 20th Century is due to failure of its eradication completely. Parasite recurrence occurs due to high densities of parasite, low immunity and non opimized drug concentration. The ineffective eradications strategies were due to indefinable complex life cycle of Plasmodium and emergence of drugs resistant strains of Plasmodium falciparum (Pf) including Artemisinin and Artemisinin based combination therapy (ACT). The vector of the disease i.e. mosquitoes became resistive towards Pyrethroids, which are only class of insecticides recommended for vector control. Artemisinin based combination therapy gained acceptance as an effective approach to counter the spread of disease resistance to chloroquine, sulfadoxine, pyrimethamine and other anti malarial drugs. Understanding the underlying molecular basis of the pathogenesis led to the development of some new diagnostic, drugs and insecticides. Reports on the use of new combination therapies reduced the burden of disease worldwide. Some of the new combination therapies are in clinical stage of development that have efficacy against drug resistant parasites and the potential to use in single dose regimens to improve compliance. The current review represents the recent anti-malarial research carried out globally especially in the class of synthesis of small molecule and natural product derivatives as potent anti-malarial drugs. The review also covers the advancement in the anti-malarial vaccine development although goal for vaccine development still remains elusive.

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An efficient and direct access to thiazolidinone is developed. 2-Thiazolidinone is synthesized by urea and 2-Aminoethylmercaptan hydrochloride and this one-step process proceeds with good yields, under mild conditions. The structure of the compound was confirmed by IR, 1H NMR, MS and the product purity was 98 % by HPLC.

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Background: N-Heterocycles are of special interest because, many natural and synthetic bioactive compounds are found to be N-containing heterocycles and they constitute an important class of pharmacophores in medicinal chemistry. Recently, 1,2,3-triazoles have been found to possess a vast range of vital applications in the agrochemical, pharmaceutical, and materials field. In addition, various compounds of the 1,2,3-triazole family have shown a broad spectrum of biological properties such as antibacterial, and anti-HIV activity. 1,3,4- Oxadiazoles are important oxygen and nitrogen containing heterocyclic compounds, they possess desirable electronic and charge-transport properties. Methods: Two mammalian cell lines were grown in RPMI-1640 medium, supplemented with 10% heat inactivated FBS, 50 units/mL of penicillin and 50 g/mL of streptomycin and maintained at 37 C in a humidified atmosphere containing 5% CO2. The cells were maintained as ?monolayer culture? by serial sub-culturing. Preliminary cytotoxicity was performed using SRB method. Results: Sebacoyl chloride and decanedihydrazide dihydrochloride are utilized as versatile building blocks to annulate a series of novel azole and/ or azine systems. The in vitro anti-tumor activities of the synthesized compounds were evaluated against human breast cancer cell line (MCF-7) and human cervical cancer cell line (HeLa). The obtained data indicated that the majority of the tested compounds possess significant anti-tumor activities against the tested tumor cell lines. Conclusion: Sebacoyl chloride, decanedihydrazide dihydrochloride and N-nucleophiles are useful precursors for the synthesis of different functionalized N- heterocycles. The cytotoxic study revealed that the majority of the tested compounds possess significant anti-tumor activity towards the tested tumor cell lines.

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The present invention provides a kind of benzimidazole derivatives, have the formula (I) has a structure shown in; wherein R1 And R2 Independently selected from hydrogen, halogen, alkyl, alkoxy, halogenated alkyl, nitro and nitrile in the a; R3 For carboxyl, alkyl, phenyl or cyano; m of the value range is 0 – 3; n of the value range is 0 – 3; X is CH or nitrogen; Y is CH2 Or carbonyl. The invention discloses a benzimidazole derivative to a topoisomerase II activity of very strong restraining effect, therefore, can be used as a topoisomerase II inhibitor. The study found that, said compound of the invention is Topo II catalytic inhibitors. Therefore, can be used for preparing topoisomerase II as the target of the anti-tumor drug. At the same time, said styrene and imidazole derivatives to the multi-tumor cells has good […] activity, so this invention the benzimidazole derivatives can be used for the preparation of anti-cancer drug. (by machine translation)

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The purpose of the present study was to isolate and identify 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester compound from Pericampylus glaucus and to evaluate their effects on blood glucose and lipid profiles in diabetic rats. The isolation and identification of compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester was undertaken through column chromatography followed by GCMS and1HNMR. The anti-hyperglycemic effect of isolated compound was carried out against STZ-induced diabetic rats. GC followed by MS and1HNMR indicate the presence of compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester in sample. The weight was 234, retention time 2.99, and total area was 1015482. The compound significantly (P < 0.01) reduced blood glucose level in hyperglycemic rats as matched to control. The attenuation on blood glucose level with 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester were non-significant (P > 0.05) up to 4 h that became significant (P < 0.01) at 24 h as matched to diabetic group. A significant (P < 0.001) attenuation in levels of cholesterol, triglycerides, LDL and significant (P < 0.01) increased in HDL was noted in 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester treated group. The findings of this study indicate that isolated compound Pericampylus glaucus compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester has significant attenuation effect on blood glucose and lipid profiles. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Quality Control of Thiazolidin-2-one, you can also check out more blogs about2682-49-7

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The invention relates to nitrogen- and sulfur-­containing heterocyclic compounds of the formula (I), wherein, Ar represents an optionally mono- or polysubstituted aryl or heteroaryl group;, R¹ represents a carbonyl or (C2 6alkenyl)-­carbonyl group;, R² represents a hydrogen atom, or a C1 6alkyl, phenyl or phenyl(C1 4alkyl) group;, R³ represents a hydrogen atom or a (C1 6 alkoxy)carbonyl group;, R4 and R5, which may be the same or different, represent a hydrogen atom or a C1 6alkyl group;, R6 represents a hydrogen atom or a C1 6alkyl group or halophenyl group;, m is 0 or 1; and, n is 1 or 2,with the proviso that R² is a hydrogen atom when m is 0, and acid addition salts of the compounds of formula (I) and pharmaceutical compositions thereof. The invention also relates to processes for the preparation of these compounds. The compounds of formula (I) show a significant cerebral antihypoxic activity.

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A simple and practical protocol for the cross-coupling of methanesulfonamide and aryl iodides under ligand-free copper(I)-oxide-catalyzed conditions in water is reported. The method allows the preparation of a wide variety of synthetically useful N-arylated methanesulfonamides in good to excellent yields (up to 90 %) under the optimized conditions.

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The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

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A convergent stereoselective synthesis of the potent anti-inflammatory, proresolving and neuroprotective lipid mediator protectin D1 (2) has been achieved in 15% yield over eight steps. The key features were a stereocontrolled Evans-aldol reaction with Nagao’s chiral auxiliary and a highly selective Lindlar reduction of internal alkyne 23, allowing the sensitive conjugated E,E,Z-triene to be introduced late in the preparation of 2. The UV and LC/MS-MS data of synthetic protectin D1 (2) matched those obtained from endogenously produced material.

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Covering: January 2013 to September 2018 Sulfur-containing natural products are a large class of significant functional molecules. Many of these compounds exhibit potent biological activities and pharmacological properties; in fact, some of them have been developed into important drugs. The total synthesis of sulfur-containing natural products is a subject that has long attracted significant attention from synthetic organic chemists; to achieve this goal, various methods have been developed over the past years. This review surveys total syntheses of sulfur-containing natural products that introduce sulfur atoms using different sulfurization agents to construct related sulfur-containing moieties.

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