- Synthesis, characterization, DFT, docking studies and molecular dynamics of some 3-phenyl-5-furan isoxazole derivatives as anti-inflammatory and anti-ulcer agents
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A vast number of nitrogen heterocyclic derivatives comprising oxygen atom is considered as a valuable combination of therapeutic agents in curative chemistry. In particular, isoxazole, a five-member heterocyclic ring, is detected along with some of the ma
- M, Pallavi H,Al-Ostoot, Fares Hezam,Vivek, Hamse Kameshwar,Khanum, Shaukath Ara
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- The Use of Modified Clay as an Efficient Heterogeneous and Ecofriendly Catalyst for the Synthesis of Chalcones via Claisen-Schmidt Condensation
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Abstract: Clay modified by potassium fluoride (KF-modified clay) was used as an ecological alternative and heterogeneous catalyst for the preparation of chalcones via Claisen-Schmidt condensation. In this paper, we have synthesized classical chalcones by condensation of benzaldehyde substituents with acetophenone. Moreover, the other chalcones were also synthesized during the condensation of benzaldehyde substituents with 2-acetylfuran. All the results obtained show that our material can be used as an effective catalyst for the synthesis of chalcones with good yield included between 90 and 99%. The catalyst recycle study shows that the modified clay can be reused four times without a decrease in catalytic activity.
- Bentahar, S.,Dbik, A.,Khomri, M. El,Lacherai, A.,Messaoudi, N. El,Sabour, A.,Taleb, M. Ait
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p. 983 - 990
(2020/08/24)
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- Synthesis and anti-proliferative assessment of triazolo-thiadiazepine and triazolo-thiadiazine scaffolds
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A series of triazolo-thiadiazepines 4a-k were synthesized with excellent yields using dehydrated PTSA as a catalyst in toluene. Two triazolo-thiadiazines were obtained; 8a was formed directly by reflux in ethanol, whereas, PTSA promoted the formation of 8
- Boraei, Ahmed T.A.,Ghabbour, Hazem A.,Gomaa, Mohamed S.,El Ashry, El Sayed H.,Barakat, Assem
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- Design, synthesis of novel furan appended benzothiazepine derivatives and in vitro biological evaluation as potent VRV-PL-8a and H+/K+ ATPase inhibitors
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A series of new of furan derivatised [1,4] benzothiazepine analogues were synthesized starting from 1-(furan-2-yl)ethanone. 1-(Furan-2-yl)ethanone was converted into chalcones by its reaction with various aromatic aldehydes, then were reacted with 2-amino
- Lokeshwari, Devirammanahalli Mahadevaswamy,Rekha, Nanjappagowda Dharmappa,Srinivasan, Bharath,Vivek, Hamse Kameshwar,Kariyappa, Ajay Kumar
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supporting information
p. 3048 - 3054
(2017/06/13)
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- Furanyl Cyclic Ethers: Single and Double Diastereoselectivity in the Synthesis of 2,4-Di and 2,4,5-Trisubstituted Tetrahydropyrans
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Combining the desymmetrization of a prochiral bis-hydroxymethyl group with the epimerization of a chiral furanyl ether in a single transformation, high levels of double diastereoselectivity have been achieved in a synthesis of 2,4,5-trisubstituted tetrahy
- Cooper, Dennis A.,Robbins, Emma,Tizzard, Graham J.,Coles, Simon J.,O'Brien, Matthew
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p. 3441 - 3455
(2017/04/13)
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- Triethylamin-mediated addition of 2-aminoethanethiol hydrochloride to chalcones: Synthesis of 3-(2-aminoethylthio)-1-(aryl)-3-(thiophen-2-yl) propan-1-ones and 5,7-diaryl-2,3,6, 7-tetrahydro-1,4-thiazepines
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The triethylamin-mediated addition of 2-aminoethanethiol hydrochloride to chalcone analogs was investigated. This addition, bearing a 2-thienyl group at the 3-position, gave the only addition adduct at room temperature in 3 h, whereas the chalcones bearing the 2-furyl group at the 1-position gave an addition-cyclization product (1, 4-thiazepine) in the same conditions. The effect of the groups to the reaction was investigated by changing the 1- and 3-position groups. The chalcones bearing the 2-thienyl group at the 1-position and the others afforded the mixture of products in different ratio at rt for 0.5-24 h. Moreover, the addition-cyclization products (1,4-thiazepine) were obtained under reflux conditions in 36 h. The structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, infrared, and elemental analysis.
- Gürdere, Meliha Burcu,Eme?, Ali Cemal,Aslan, Osman Nuri,Budak, Yakup,Ceylan, Mustafa
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p. 536 - 545
(2016/05/02)
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- Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation, and ulcerogenic liability of new 1,3,5-triarylpyrazoline derivatives possessing a methanesulfonyl pharmacophore
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A new series of 1,3,5-triarylpyrazolines 13a–l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI)=10.23) and the most potent anti-inflammatory derivative (ED50-60.1μmol/kg) in comparison with celecoxib (COX-2 SI=9.29 and ED50=81.4μmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI)=0.33–1.33) than aspirin (UI=2.33) and comparable to celecoxib (UI=0.33).
- Abdellatif, Khaled R. A.,Fadaly, Wael A. A.,Azouz, Amany A.
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- Synthesis of 1,5-benzothiazepines: Part 41: Single pot synthesis and antimicrobial studies of 8-substituted-2,5-dihydro-4-(4-substituted aryl)-2-(2-furyl)-1,5-benzothiazepines
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8-Substittued-2,5-dihydro-4-(4-chlorophenyl/nitrophenyl)-2-(2-furyl)-1,5- benzothiazepines have been synthesized by the reaction of 5-substituted-2- aminobenzenethiols with αβ-unsaturated carbonyl compounds, such as 1-(4- chlorophenyl)-3-(2-furyl)-2-propenone and 3-(2-furyl)-1-(4-nitrophenyl)-2-propenone in dry ethanol saturated with dry HCl and in dry toluene containing trifluoroacetic acid respectively, in 52-65% yields. The products were characterized by microestimations for C,H and N and by spectral studies comprising IR, 1H NMR and mass spectral studies. All the synthesized compounds have been screened for their antimicrobial activity against Gram-positive bacteria, Staphylococcus aureus, Gram-negative bacteria, Pseudomonas aeruginosa and fungi, Candida albicans and Aspergillus niger. Most of the compounds exhibited good antifungal activity.
- Pant, Seema,Avinash,Yadav, Meenakshi
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p. 381 - 386
(2019/01/21)
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- Synthesis and In Vitro Antifungal Evaluation of 1,3,5-Trisubstituted-2-Pyrazoline Derivatives
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Pyrazolines, the well-known five-membered nitrogen-containing heterocyclic compounds, have received considerable interests in the fields of medicinal and agricultural chemistry because of their broad spectrum of biological activities. To discover more pot
- Deng, Hui,Yu, Zhi-Yi,Shi, Guan-Ying,Chen, Ming-Jing,Tao, Ke,Hou, Tai-Ping
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experimental part
p. 279 - 289
(2012/05/20)
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- Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones
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Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are collectively known as chalcones. The cytotoxic potential of chalcones which consists of C6-C 3-C6 units gets enhanced by the incorporation of pyrazole ring as proved by our earlier studies. Thus in the present work, pyrazoles of chalcones with ring A substituted by furan, naphthalene and variety of substituted phenyl rings has been prepared and evaluated for in vitro cytotoxic activity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines. Springer Science+Business Media, LLC 2011.
- Nepali, Kunal,Kadian, Kanika,Ojha, Ritu,Dhiman, Rajni,Garg, Atul,Singh, Gagandip,Buddhiraja, Abhishek,Bedi, Preet Mohinder Singh,Dhar, Kanaya Lal
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p. 2990 - 2997
(2012/10/29)
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- A rational approach for the design and synthesis of 1-acetyl-3,5-diaryl-4, 5-dihydro(1H)pyrazoles as a new class of potential non-purine xanthine oxidase inhibitors
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Xanthine oxidase is a complex molybdoflavoprotein that catalyses the hydroxylation of xanthine to uric acid. Fifty three analogues of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles were rationally designed and synthesized and evaluated for in vitro xanthine
- Nepali, Kunal,Singh, Gurinderdeep,Turan, Anil,Agarwal, Amit,Sapra, Sameer,Kumar, Raj,Banerjee, Uttam C.,Verma, Prabhakar K.,Satti, Naresh K.,Gupta, Manish K.,Suri, Om P.,Dhar
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experimental part
p. 1950 - 1958
(2011/04/27)
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- Anti-bacterial and anti-leishmanial studies of 4, 6-diarylpyrimidin-2- amines
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Seven new chalcones along with nine already reported ones were synthesized from aryl aldehydes and substituted acetophenones by Claisen-Schmidt condensation. Each chalcone was treated with guanidine hydrochloride followed by oxidation with H2O
- Bukhari, Mujahid Hussain,Siddiqui, Hamid Latif,Ashraf, Chaudhary Muhammad,Hussain, Tanvir
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scheme or table
p. 720 - 725
(2012/06/18)
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- Tandem [4 + 1 + 1] annulation and metal-free aerobic oxidative aromatization: Straightforward synthesis of highly substituted phenols from one aldehyde and two ketones
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Polysubstituted phenols are efficiently assembled from one aldehyde and two different methyl ketones in a one-pot operation via a newly base-induced regiospecific [4 + 1 + 1] annulation and sequential metal-free oxidative aromatization using molecular oxygen (from air) as the sole oxidant at room temperature.
- Wang, Mang,Fu, Zhenqian,Feng, Hui,Dong, Ying,Liu, Jun,Liu, Qun
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supporting information; experimental part
p. 9061 - 9063
(2011/02/17)
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- Atom-efficient, solvent-free, green synthesis of chalcones by grinding
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An improved Claisen-Schmidt condensation reaction of methyl ketones and aromatic aldehydes can be achieved by grinding at room temperature in the absence of solvents. This process is simple, efficient, economical, and environmentally benign compared to classical reactions.
- Rateb, Nora M.,Zohdi, Hussein F.
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experimental part
p. 2789 - 2794
(2009/12/06)
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