- Activated charcoal-mediated synthesis of chalcones catalyzed by NaOH in water
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A variety of chalcones were synthesized in good yields by the activated charcoal-mediated aldol reactions between benzaldehydes and acetophenones catalyzed by NaOH in water. 2,6-Bis((E)-benzylidene)cyclohexan-1-ones were prepared by the aldol reactions between benzaldehydes and cyclohexanone. Activated charcoal could be recycled five times without the significant decrease of yields.
- Tanemura, Kiyoshi,Rohand, Taoufik
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supporting information
(2021/02/27)
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- Novel benzothiazole based sulfonylureas/sulfonylthioureas: Design, synthesis and evaluation of their antidiabetic potential
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In the present study, twenty-eight benzothiazole based sulfonylureas/sulfonylthioureas were synthesized and were assessed for their antidiabetic effect in a normoglycemic rat model by the in vivo oral glucose tolerance test (OGTT). All the synthesized com
- Kharbanda, Chetna,Alam, Mohammad Sarwar,Hamid, Hinna,Javed, Kalim,Bano, Sameena,Ali, Yakub,Dhulap, Abhijeet,Alam, Parwez,Pasha
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p. 6777 - 6786
(2016/08/10)
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- Synthesis, characterization of 4,6-disubstituted aminopyrimidines and their sulphonamide derivatives as anti-Amoebic agents
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The present study describes the synthesis and anti-Amoebic activity of 4,6-disubstituted aminopyrimidines (1b-10b) and their sulphonamide derivatives (1-20). All the desired compounds were characterized by spectral data and their purity was confirmed by e
- Siddiqui, Shadab Miyan,Azam, Amir
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p. 2976 - 2984
(2014/05/06)
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- Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents
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The present study aims at the synthesis of pyrazolines bearing benzothiazole and their evaluation as anti-inflammatory agents. The synthesized compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model. Two co
- Kharbanda, Chetna,Alam, Mohammad Sarwar,Hamid, Hinna,Javed, Kalim,Bano, Sameena,Dhulap, Abhijeet,Ali, Yakub,Nazreen, Syed,Haider, Saqlain
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p. 5804 - 5812
(2015/02/02)
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- Silicotungstic acid catalysed Claisen Schmidt condensation reaction: An efficient protocol for synthesis of 1,3-diaryl-2-propenones
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An efficient and clean synthesis of 1,3-diaryl-2-propenones has been carried out by Claisen Schmidt condensation reaction of aryl methyl ketones with a series of aromatic aldehydes at room temperature in the presence of the catalyst silicotungstic acid (STA). This method provides an ecofriendly, chemoselective, efficient and green synthesis of 1,3-diaryl-2-propenones in excellent yields.
- Rajput, Jaspreet Kaur,Kaur, Gagandeep
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experimental part
p. 646 - 649
(2012/02/15)
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- Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro
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A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.
- Parekh, Shrey,Bhavsar, Dhairya,Savant, Mahesh,Thakrar, Shailesh,Bavishi, Abhay,Parmar, Manisha,Vala, Hardevsinh,Radadiya, Ashish,Pandya, Nilay,Serly, Juliana,Molnár, Joseph,Shah, Anamik
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scheme or table
p. 1942 - 1948
(2011/04/26)
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- Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion
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The high levels of hepatitis B virus (HBV) surface antigen (HBsAg)-bearing subviral particles in the serum of chronically infected individuals play an important role in suppressing HBV-specific immune response and are only mildly affected by the current small molecule therapies. Thus, a therapy that specifically reduces HBsAg serum levels could be used in combination therapy with nucleos(t)ide drugs or permit therapeutic vaccination for the treatment of HBV infection. Herein, we report the design, synthesis, and evaluation of novel triazolo-pyrimidine inhibitors (1, 3, and 4) of HBsAg cellular secretion, with activity against drug-resistant HBV variants. Extensive SAR led to substantial improvements in the EC50 of the parent compound, 5 (HBF-0259), with the best being 3c, with EC50 = 1.4 ± 0.4 μM, SI ≥ 36. The lead candidates, both 1a (PBHBV-001) and 3c (PBHBV-2-15), were well-tolerated in both normal and HBV-transgenic mice and exhibited acceptable pharmacokinetics and bioavailability in Sprague-Dawley rats.
- Yu, Wenquan,Goddard, Cally,Clearfield, Elizabeth,Mills, Courtney,Xiao, Tong,Guo, Haitao,Morrey, John D.,Motter, Neil E.,Zhao, Kang,Block, Timothy M.,Cuconati, Andrea,Xu, Xiaodong
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supporting information; experimental part
p. 5660 - 5670
(2011/10/08)
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- Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors
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Fatty acid biosynthesis is essential for bacterial survival. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and -negative bacteria. Fifty-six 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 1-(5-(4-fluorophenyl)- 3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (12) and 1-(5-(4-chlorophenyl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (13) were potent inhibitors of E. coli FabH.
- Lv, Peng-Cheng,Sun, Juan,Luo, Yin,Yang, Ying,Zhu, Hai-Liang
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scheme or table
p. 4657 - 4660
(2010/09/16)
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- Syntheses of 1,5-benzothiazepines: Part XXXVI - Syntheses and antimicrobial evaluation of 2-(2-chlorophenyl)-4-(4-chlorophenyl/2-thienyl)-2,5-dihydro-8- substituted-1,5-benzothiazepines
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Six 5-substituted-2-aminobenzenethiols have been reacted with 3-(2-chlorophenyl)-1-(4-chlorophenyl)-2-propenone and 3-(2-chlorophenyl)-1-(2- thienyl)-2-propenone in dry ethanol saturated with dry HCl gas, to obtain twelve new compounds, 8-substituted-2-(2-chlorophenyl)-4-(4-chlorophenyl/2-thienyl)-2, 5-dihydro-1,5-benzothiazepines in satisfactory yields. The structures of the final products have been assigned by elemental microanalyses data for elements, C, H, and N and by IR, 1H NMR, and mass spectroscopies. The synthesized compounds have been evaluated for their relative antimicrobial activity against the gram-positive bacteria, Staphylococcus aureus, gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The compounds have been found to show little antibacterial activity, but interestingly, showed significant antifungal activity. Copyright Taylor & Francis Group, LLC.
- Pant, Seema,Sharma, Priyanka,Pant, Umesh C.
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scheme or table
p. 2974 - 2983
(2009/09/06)
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