- An efficient one-pot synthesis of pyridazinones and phthalazinones using HY-zeolite
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Figure represented. The first one-pot synthesis of pyridazinones and phthalazinones from arenes, cyclic anhydrides, and ArNHNH2 in the presence of efficient recyclable heterogeneous catalyst, HY-zeolite, in high yield and short reaction time is reported.
- Zare, Leila,Mahmoodi, Nosratollah,Yahyazadeh, Asieh,Mamaghani, Manouchehr,Tabatabaeian, Khalil
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Read Online
- Extracting agent and preparation method thereof, and method for separating rare earth elements including yttrium and lanthanides
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The invention belongs to the field of rare earth resource recovery, and provides an extracting agent. The extracting agent comprises alkyl phenyl oxobutyric acid. The alkyl phenyl oxobutyric acid comprises one or more compounds with structures as shown in
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Paragraph 0079-0086
(2021/03/31)
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- Synthesis, anti-convulsant activity and molecular docking study of novel thiazole pyridazinone hybrid analogues
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Pyridazinone analogues have been known to be potential candidates for anticonvulsant agents. We have identified several pyridazinone-based anticonvulsant agents. As a continuation to our previous research, a series of hybrid pyridazinone-thiazole connected through amide linkage were designed and synthesized. Among these, compound SP-5F demonstrated significant anticonvulsant activity with median effective dose of 24.38 mg/kg (MES) and 88.23 mg/kg (scPTz). Results of GABA estimation showed a marked increase in the GABA level when compared with control. Molecular docking studies at the active site of GABA receptor, further confirmed the GABA modulatory effects of SP-5F.
- Khisal, Subuhi,Mishra, Ravinesh,Partap, Sangh,Siddiqui, Aness Ahmad,Yar, Mohammad Shahar
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- An Electrophilic Trifluoromethylthiolation of Silylenol Ethers and β-Naphthols with Diethylaminosulfur Trifluoride and (Trifluoromethyl)trimethylsilane
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An efficient and general trifluoromethylthiolation of silylenol ethers and β-naphthols have been accomplished employing the combination of diethylaminosulfur trifluoride (DAST) and (trifluoromethyl)trimethylsilane (CF3TMS) as source of electrophilic trifluoromethylthio moiety for the synthesis of α-trifluoromethylthiolated carbonyl compounds and β-naphthols in good yields. Important features of this method include wide functional group tolerance and use of readily available DAST/CF3TMS. Potential of the methodology was demonstrated via the synthesis of α-trifluoromethylthiolated (+)-4-cholesten-3-one and naphthoquinone. (Figure presented.).
- Saravanan, Perumal,Anbarasan, Pazhamalai
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supporting information
p. 2894 - 2899
(2018/08/17)
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- Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents
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A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABAA receptor.
- Partap, Sangh,Yar, Mohammad Shahar,Hassan, Md. Zaheen,Akhtar, Md. Jawaid,Siddiqui, Anees A.
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- Enzymatic synthesis of chiral γ-amino acids using ω-transaminase
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In this study, we successfully synthesized enantiomerically pure (R)- and (S)-γ-amino acids (>99% ee) using ω-transaminase (ω-TA) through kinetic resolution and asymmetric synthesis respectively. The present study demonstrates the high potentiality of ω-TA reaction for the production of chiral γ-amino acids.
- Shon, Minsu,Shanmugavel, Ramachandran,Shin, Giyoung,Mathew, Sam,Lee, Sang-Hyeup,Yun, Hyungdon
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supporting information
p. 12680 - 12683
(2015/05/20)
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- Ultrasound-promoted Friedel-Crafts acylation of arenes and cyclic anhydrides catalyzed by ionic liquid of [bmim]Br/AlCl3
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A simple and efficient method of Friedel-Crafts acylation of arenes with succinic anhydride, phthalic anhydride and glutaric anhydride under the action of 1-butyl-3-ethylimidazolium ([bmim]Br/AlCl3 ([bmim]+) cation (ionic liquid) and ultrasound irradiation is presented. Thy purity of products was tested by GC-MS and their structures evaluated by IR and 1H NMR spectroscopy.
- Fekri, Leila Zare,Nikpassand, Mohammad
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p. 1825 - 1829
(2015/01/09)
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- Synthesis and biological evaluation of some novel sulfamoylphenyl- pyridazinone as anti-inflammatory agents (Part-II)
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Seven novel 6-aryl-2-(p-sulfamoylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-g) were synthesized by the condensation of appropriate aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Structure of all compounds have been elucidated by elemental analysis, IR, 1H NMR, 13C NMR, DEPT and MS spectrscopy. These compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 2b exhibited anti-inflammatory activity comparable to that of celecoxib (at 5h). Two other compounds 2d and 2g showed promising anti-inflammatory activity (edema reduction more than 80% at 5h). These compounds (2b, 2d and 2g) did not produce any ulceration in gastric region.
- Bashir, Rafia,Yaseen, Shafiya,Ovais, Syed,Ahmad, Shamim,Hamid, Hinna,Alam,Samim, Mohammad,Javed, Kalim
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experimental part
p. 92 - 96
(2012/05/19)
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- Search for new pharmacophore as antimalarial agent: Synthesis and antimalarial activity of some 2(3H)-furanones bearing quinoline moiety
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A series of substituted 3-[(substituted-2-chloroquinolin-3-yl)methylene]-5- (substituted-phenyl)-furan-2(3H)-ones (4a-p) have been synthesized and evaluated for their in vitro antimalarial activity against P. falciparum. The title compounds were synthesized by condensing 3-(substituted-benzoyl)propionic acids (3a-d) with substituted 2-chloroquinoline-3-carbaldehydes (2a-d) following modified Perkin's reaction. Compounds 3-[2-chloro-6-methylquinolin-3-yl) methylene]-5-(2,4-dimethyl-phenyl)-furan-2(3H)-one (4n) and 3-[2-chloro-6- methoxyquinolin-3-yl)methylene]-5-(2,4-dimethyl-phenyl)-furan-2(3H)-one (4p) showed promising antimalarial activity with MIC of 10 μg/mL.
- Alam, Mohammad Mumtaz,Sarkar, Deba Priya,Alam, Ozair,Husain, Asif,Marella, Akranth,Akhtar, Mymoona,Shaquiquzzaman, Mohammad,Khanna, Suruchi
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scheme or table
p. 231 - 236
(2011/10/09)
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- Synthesis of quinoline-attached furan-2(3H)-ones having anti-inflammatory and antibacterial properties with reduced gastro-intestinal toxicity and lipid peroxidation
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A series of 5-aryl-3-[(2-chloroquinolin-3-yl)methylene] furan-2(3H)- ones (3a-p) were synthesized. The required 3-(substituted benzoyl)propionic acids 2a-d were prepared under Fried?l-Crafts acylation reaction conditions. The substituted 2-chloroquinoline-3-carboxaldehydes 1a-d were synthesized by reaction of substituted phenylethanone oxime with phosphorus oxychloride in presence of dimethylformamide using the Vilsmeier-Haack reaction method. These compounds were screened for their anti-inflammatory and antibacterial activities along with their ulcerogenic and lipid peroxidation potentials. The compounds that showed significant anti-inflammatory activity were further screened for their analgesic activity. The compounds were less toxic in terms of ulcerogenicity as compared to a standard, which was also supported by lipid peroxidation studies. The antibacterial activities were performed against Staphylococcus aureus and Escherichia coli. Compounds 3f, 3n and 3o showed significant activity against both S. aureus and E. coli having an minimum inhibitory concentration (MIC) value of 6.25 μg mL-1. Copyright 2011 (CC) SCS.
- Alam, Mohammad M.,Sarkar, Deba Priya,Husain, Asif,Marella, Akranth,Shaquiquzzaman, Mohammad,Akhter, Mymoona,Shaharyar, Mohammad,Alam, Ozair,Azam, Faizul
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experimental part
p. 1617 - 1626
(2012/05/05)
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- Amide derivatives of sulfonamides and isoniazid: Synthesis and biological evaluation
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In the present study, various amide derivatives of sulfanilamide, sulfamethoxazole, sulfadiazine, dapsone and isoniazid have been synthesized by condensing them with appropriate 4-oxo-4-(4-substituted phenyl)butanoic acid moiety. The compounds have been evaluated for their antiinflammatory, ulcerogenic and antibacterial activities. Their structures were established on the basis of elemental analysis, 1H NMR and mass spectral data. Some of the compounds were found to have significant antiinflammatory and antibacterial activities. Additionally, these derivatives were low in their ulcerogenic action, which is the main side effect of commonly used NSAIDs.
- Husain, Asif
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experimental part
p. 513 - 521
(2010/01/16)
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- Aroylpropionic acid based 2,5-disubstituted-1,3,4-oxadiazoles: Synthesis and their anti-inflammatory and analgesic activities
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Synthesis and biological evaluation of various aroylpropionic acid derivatives containing 1,3,4-Oxadiazole nucleus is reported here. The compounds (3a-w) were synthesized by cyclization of 3-aroylpropionic acids into 1,3,4-oxadiazole nucleus by treating with various aryl acid hydrazides in the presence of POCl3. The structures of new compounds are supported by IR, 1H NMR and MS data. These compounds were tested in vivo for their anti-inflammatory activity. All the compounds tested showed anti-inflammatory activity. The compounds which showed activity comparable to the standard drug ibuprofen were screened for their analgesic, ulcerogenic and lipid peroxidation activities. Seven (3c, g, i, j, m, o, p) out of 23 new compounds showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test with very less ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde production (MDA), which is one of the byproducts of lipid peroxidation. Compound 3i and o showed 89.50 and 88.88% of inhibition in paw edema, 69.80 and 66.25% protection against acetic acid induced writhings and 0.7 and 0.65 of severity index respectively, compared to 90.12, 72.50 and 1.95 values of ibuprofen. The study showed that the cyclization of carboxylic group of aroylpropionic acids into an oxadiazole nucleus resulted in compounds having good anti-inflammatory and analgesic effects with reduced gastric irritation.
- Akhter, Mymoona,Husain, Asif,Azad, Bismillah,Ajmal
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scheme or table
p. 2372 - 2378
(2009/12/03)
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- Studies on butenolides: 2-Arylidene-4-(substituted aryl)but- 3-en-4-olides - Synthesis, reactions and biological activity
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2-Arylidene-4-(substituted aryl)but-3-en-4-olides also known as 3 -arylidene-5-(substituted aryl)-2(3H)-furanones have been prepared from 3-(substituted aroyl) propionic acid and aromatic aldehydes. Some of the selected butenolides have been reacted with ammonia and benzylamine to give corresponding pyrrolones and N-benzylpyrrolones respectively and characterized on the basis of 1H NMR and Mass spectrometric data and elemental analysis results. These compounds have been tested for anti-inflammatory and antimicrobial actions.
- Khan,Husain,Sharma
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p. 2160 - 2171
(2007/10/03)
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- Process for the production of cyclic sulfonium salts
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A process for the production of a 5-7 membered ring cyclic sulfonium salt compound, including a 5-7 membered ring cyclic sulfonium salt compound having a non-nucleophilic anion, is described. Members of the latter group are potentially useful as initiators for cationic polymerizations. The process comprises reacting a 1.4-, 1.5-, or 1.6-diol compound or a 5-7 membered ring cyclic ether compound with a mercapto compound and a strong protonic acid yielding the cyclic sulfonium salt compound. Some compounds described are also novel compounds per se.
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- Syntheses of Tetrahydronaphthalenes. Part II
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Syntheses utilizing the cyclodehydration method to prepare novel tetrahydronaphthalenes substituted with functional groups at each position of the aromatic ring and various alkyl groups at the 1-position of the non-aromatic ring are described.
- Parlow, John J.
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p. 3297 - 3314
(2007/10/02)
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