M. M. H. Arief

Validation of quantitative method for azoxystrobin residues in green beans and peas.

This study presents a method validation for extraction and quantitative analysis of azoxystrobin residues in green beans and peas using HPLC-UV and the results confirmed by GC-MS. The employed method involved initial extraction with acetonitrile after the addition of salts (magnesium sulfate and sodium chloride), followed by a cleanup step by activated neutral carbon. Validation parameters; linearity, matrix effect, LOQ, specificity, trueness and repeatability precision were attained. The spiking levels for the trueness and the precision experiments were (0.1, 0.5, 3 mg/kg). For HPLC-UV analysis, mean recoveries ranged between 83.69% to 91.58% and 81.99% to 107.85% for green beans and peas, respectively. For GC-MS analysis, mean recoveries ranged from 76.29% to 94.56% and 80.77% to 100.91% for green beans and peas, respectively. According to these results, the method has been proven to be efficient for extraction and determination of azoxystrobin residues in green beans and peas.

Chemistry of Phosphorus Ylides. Part 34 Synthesis of Chromenone Phosphanylidene and Cyclobutylidene Derivatives

Abstract The reaction of nucleophilic phosphacumulene ylides with visnaginone and khellinone afforded the corresponding phosphanylidene and furochromene derivatives. Moreover, pyranochromenes were obtained from the reaction of chromene carbaldehydes with phosphacumulenes. On the other hand, the phosphanylidene-cyclobutylidenes and their dimers were produced from the reaction of furochromene carbaldehydes with the same phosphonium reagents. GRAPHICAL ABSTRACT

SYNTHESIS OF SOME SACCHARIN DERIVATIVES OF EXPECTED BIOLOGICAL ACTIVITY BASED ON N-(SACCHARINYL)-ACETIC ACID AZIDE

Abstract Azide was prepared from the corresponding acid chloride . The base catalyzed decomposition with aromatic amines, aminobenzoic acids and/or hydrazines afforded the corresponding anilides and/or hydrazides via azido group displacement. Compounds and were refluxed in Ac2O to give 1,3,4-oxadiazole derivatives and . Lewis acid catalyzed decomposition of azide with anhyd. AlCl3 in dry aromatic substrates gave the corresponding ketones . Also, the reaction of azide with glycine gave .

α,β-Unsaturated γ-Oxo Carboxylic Acids in Heterocylic Synthesis II. Behavior of 4-(5,5-Dioxodibenzothiophen-2-yl)-4-oxo-2-butenoic Acid Towards Carbon Nucleophiles under Michael Reaction Condition

4-(5,5-Dioxodibenzothiophen-2-yl)-4-oxo-2-butenoic acid ( 1 ) was condensed with compounds containing active methylene groups under Michael reaction conditions to form the Michael adducts 2a-c , 3a-c , and 4a-b . The behavior of Michael adduct towards the action of hydrazine hydrate was investigated. The compounds were tested for biological properties.

INVESTIGATION ON SOME REACTIONS OF SACCHARINYL BENZOIC ACID AZIDES

Abstract Saccharinyl benzoic acid azides 2a-c were used to synthesize a number of noncondensed heterocyclic systems. Thus azides 2a or 2c reacted with glycine to give 1,3-oxazolin-5-one derivatives 3a and 3b. However azide 2b reacted to give diaryl urea derivative which was easily cyclized to give imidazol -2,5- dione (6). Also azides 2a-c reacted with glycolic acid to give 1,3-oxazolin -2,5-dione derivatives (7a-c) and with aroyl hydrazines to give the corresponding hydrazides (8a-f) which were cyclized to 1,3,5-oxadiazole derivatives (9a-f).

STUDIES ON α-[6-(2′-METHOXYNAPHTHALENYL)-4-PHENYLPYRIMIDINYLTHIO]-β/-(4-PHENYLBENZOYL)PROPIONIC ACID AND THE BIOLOGICAL ACTIVITY OF SOME PRODUCTS

Abstract β-(4-phenylbenzoyl)acrylic acid I reacted with 6-(2′-methoxynaphthalenyl)-4-phenylpyrimidine-2(1H)thione to furnish α-[6-(2′-methoxynaphthalenyl)-4-phenylpyrimidinylthio]-β-(4-phenylbenzoyl)propionic acid II. Dehydration of acid II aforded furanone derivative III. The behaviour of III towards hydrazine hydrate, hydroxylamine hydrochloride, primary amines, aromatic hydrocarbons (under Friedel-Crafts conditions) and carbon nucleophiles (under Grignard conditions) has been investigated.

Microwave synthesis and fluorescence properties of homo- and heterodimeric monomethine cyanine dyes TOTO and their precursors

ABSTRACT A series of monomeric and dimeric cyanine dyes belonging to the thiazole orange family have been prepared via an improved synthetic procedure, by the reaction of the monomethine dye containing an iodoalkyl group with tertiary diamine linkers under microwave irradiation. The effects of microwave power and irradiation time on yield were examined. The electronic absorption and steady-state fluorescence spectra of prepared dyes have been investigated. Fluorescence properties indicate significance in singlet oxygen sensitization and make the present compounds potential candidates in the area of photodynamic therapy. GRAPHICAL ABSTRACT

Recent Advances in the Medicinal Chemistry of Liver X Receptors

Nuclear hormone receptors represent a large family of ligand-activated transcription factors that include steroid receptors, thyroid/retinoid receptors, and orphan receptors. Among nuclear hormone receptors, the liver X receptors have emerged as very important drug targets. These receptors regulate some of the most important metabolic functions, and they were also identified as anti-inflammatory transcription factors and regulators of the immune system. The development of drugs targeting liver X receptors continues to be a challenge, but advances in our knowledge of receptor structure and function move us forward, toward achieving this goal. This review highlights the latest advances in the development of synthetic LXR modulators in the primary literature from 2013 to 2017. In this review, we place great emphasis on the structure and function of LXRs because of their essential role in the drug design process. The structure-activity relationships of the most active and promising synthetic modulators are discussed.

γ-Oxo Carboxylic Acids in Heterocyclic Synthesis, III. Synthesis of Biologically Active 4-Benzylamino-6-(5,5-dioxodibenzothiophen- 2-yl)-2,3,4,5-tetrahydropyridazin-3-ones

α-Benzylamino-β-(5,5-dioxodibenzothiophen-2-carbonyl)propionic acid (1) has been synthesized by treating the corresponding β-aroylacrylic acid with benzylamine in dry benzene. On treatment with hydrazine hydrate the keto acid 1 furnishes the corresponding pyridazinone derivative 2. The behaviour of 2 towards carbon electrophiles, namely, ethyl chloroacetate, acrylonitrile, formaldehyde and secondary amines (under Mannich reaction conditions), aromatic aldehydes and carbon nucleophiles, namely, POCl3/PCl3 and P2S5 has been investigated. The 3-chloropyridazine derivative 13 reacts with hydrazine hydrate to give the 3-hydrazino derivative 14. On treatment with ethyl acetoacetate and/or acetylacetone the hydrazine 14 undergoes cyclization to afford pyrazolone derivative 16 and 3-(3,5-dimethylpyrazol- 1-yl)pyridazine derivative 17, respectively. On reaction with acetylhydrazine in boiling butanol and/or sodium azide in DMF the 3-chloropyridazine derivative 13 affords the triazolo[4,3-b]pyridazine 18 and the tetrazolo[1,5-b]pyridazine 19, respectively. The anti-microbial activity of the synthesized derivatives has been investigated.

α,β-unsaturated 4-oxo acids in heterocyclic synthesis

Abstract3-(1,1-Dioxadibenzothien-4-oyl)acrylic acid (1) was condensed with compounds containing active methylene groups under Michael reaction conditions to furnish the Michael adducts (lactones,2a–c, lactams,3a–c, ketones4a, b). The behavior of these adducts toward the action of hydrazine hydrate were investigated. The compounds were tested for their biological properties.