- 3-nitro-2H-chromenes as a new class of inhibitors against thioredoxin reductase and proliferation of cancer cells
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A series of 3-nitrochromenes were designed and synthesized. These compounds showed good inhibitory activity against thioredoxin reductase (TrxR) and the proliferation of A549 cancer cells. The structure-activity relationship analysis indicates that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. The bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity. A series of 3-nitrochromenes were designed and synthesized. They showed good inhibitory activity against thioredoxin reductase and the proliferation of A549 cancer cells. Structure-activity relationship analysis revealed that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. Bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity. Copyright
- Xiao, Guo-Qiang,Liang, Bao-Xia,Chen, Shu-Han,Ou, Tian-Miao,Bu, Xian-Zhang,Yan, Ming
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Read Online
- Synthesis, characterization, and antifungal activity of novel chromene oxadiazole based dithiocarbamates
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A series of novel conjugated chromene oxadiazole-based dithiocarbamate (5a–i) derivatives have been synthesized from oxadiazole (4a–c) intermediates with carbon disulfide. The structures of all the newly synthesized compounds were established by IR, NMR, and Mass spectral analysis. The synthesized derivatives were screened for their antifungal activity against Aspergillus niger fungal strain and the results showed that some of the derivatives were found to exhibit good antifungal activity.
- Bhoga, Srinivas,Gutam, Madhu,Konda, Santosh Kumar,Krupadanam, G. L. David,Mattela, Kutumbarao,Nayaki, Salva Reddy,Thalari, Gangadhar
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supporting information
(2022/03/02)
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- DUAL AGONISTS OF FXR AND PPARδ AND THEIR USES
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The present invention relates to small molecule compounds and their use as agonists of farnesoid X receptor (FXR) and/or peroxisome proliferator activated receptor delta (PPARδ). The present invention also relates to the use of said compounds in the treatment of metabolic diseases and respective methods of treatment.
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Page/Page column 38; 46
(2019/04/16)
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- Microwave-Assisted Rapid and Efficient Synthesis of New Series of Chromene-Based 1,2,4-Oxadiazole Derivatives and Evaluation of Antibacterial Activity with Molecular Docking Investigation
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A new series of novel chromene-based oxadiazole derivatives were synthesized from a variety of chromene-based amidoximes with readily available carboxylic acids under conventional oil bath heating as well as under microwave irradiation. The use of commercially available EDCI and HOBt as coupling reagents in DMF combined with microwave heating resulted in high yields and purities of the product 1,2,4-oxadiazoles in an expeditious manner. This methodology is successfully applied to synthesize 18 numbers of new 2H-chromene-substituted 1,2,4-oxadiazole derivatives in good to high yields. The structure of the product was ascertained by X-ray crystallographic analysis. All the synthesized compounds were evaluated for their in vitro antibacterial activity against two different pathogenic bacterial strains, that is, Escherichia coli (MTCC614) and Klebsiella pneumoniae (MTCC4031). The obtained results from in vitro antimicrobial assays indicated that 6g and 6h exhibited good antibacterial activity nearer to the standard drug, gentamicin. The molecular docking studies showed that compounds 6g and 6h show hydrogen bonding interaction with the bacterial target DNA gyrase of E.?coli.
- Baral, Nilofar,Mohapatra, Seetaram,Raiguru, Bishnu Prasad,Mishra, Nilima Priyadarsini,Panda, Pravati,Nayak, Sabita,Pandey, Satyendra Kumar,Kumar, P. Sudhir,Sahoo, Chita Ranjan
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p. 552 - 565
(2019/01/04)
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- Discovery of (S)-6-methoxy-chroman-3-carboxylic acid (4-pyridin-4-yl-phenyl)-amide as potent and isoform selective ROCK2 inhibitors
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ROCK1 and ROCK2 are highly homologous isoforms. Accumulated studies indicate that they have distinct different functions, and the development of isoform selective ROCK inhibitors will pave new roads for the treatment of various diseases. In this work, a series of amide-chroman derivatives were synthesized and biologically evaluated in order to develop potent and isoform selective ROCK2 inhibitors. Remarkably, (S)-6-methoxy-chroman-3-carboxylic acid (4-pyridin-4-yl-phenyl)-amide ((S)-7c) possessed ROCK2 inhibitory activity with an IC50 value of 3 nM and 22.7-fold isoform selectivity (vs. ROCK1). Molecular docking indicated that hydrophobic interactions were the key element for the high potency and isoform selectivity of (S)-7c. The binding free energies predicted by MM/GBSA were in good agreement with the experimental bioactivities, and the analysis of individual energy terms suggested that residue Lys105 in ROCK1 or Lys121 in ROCK2 was the key residue for the isoform selectivity of (S)-7c.
- Pan, Jinpeng,Yin, Yan,Zhao, Lianhua,Feng, Yangbo
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p. 1382 - 1390
(2019/02/26)
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- One pot, three component 1,3 dipolar cycloaddition: Regio and diastereoselective synthesis of spiropyrrolidinyl indenoquinoxaline derivatives
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A competent and highly discriminating one-pot synthesis of highly diversified novel functionalized indenoquinoxalone grafted spiropyrrolidine linked chromene-3-carbonitrile conjugates accumulating three pharmocophoric cores, heterocyclic indenoquinoxalone, pyrrolidines and chromene-3-carbonitrile in a single molecular framework by means of 1,3-dipolar cycloaddition reaction between indenoquinoxalone, proline/benzyl amine and chromene-3-carbonitrile in ethanol under classical and microwave conditions is described. The three component 1,3-dipolar cycloaddition reaction proceeds via in situ generation of azomethine ylides by the decarboxylative condensation of indenoquinoxalone with proline/benzyl amine and their selectivity towards the endo cyclic double bonds of dipolarophile (chromene-3-carbonitrile) leading to the formation of highly functionalised regio- and diastereoselective molecular hybrids. This methodology exemplifies the green chemistry protocol such as mild reaction conditions, high yields, one-pot procedure and operational simplicity.
- Pattanaik, Priyabrata,Nayak, Sabita,Ranjan Mishra, Deepak,Panda, Pravati,Prasad Raiguru, Bishnu,Priyadarsini Mishra, Nilima,Mohapatra, Seetaram,Arjunreddy Mallampudi,Purohit, Chandra Shekhar
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supporting information
p. 2688 - 2694
(2018/06/06)
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- 10-Camphorsulfonic acid ((±)-CSA) catalyzed facile one-pot synthesis of a new class of 2,5-disubstituted 1,3,4-oxadiazoles
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A convenient and efficient one-pot synthesis of 2,5-disubstituted-1,3,4-oxadizoles is described. Various carboxylic acid hydrazides reacted efficiently with different carboxylic acid chlorides and 10-camphorsulfonic acid. This methodology was successfully
- Mule, Siva Nagi Reddy,Battula, Sailaja Kumari,Velupula, Ganapathi,Guda, Dinneswara Reddy,Bollikolla, Hari Babu
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p. 58397 - 58403
(2015/02/19)
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- Synthesis and cytotoxicity evaluation of some novel 3,5-disubstituted-1,2, 4-oxadiazoles
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Novel 3,5-disubstituted 1,2,4-oxadiazoles 4a-4j were prepared from commercially available chlorosalicylaldehyde and screened for their cytotoxicity properties using brine shrimp (Artemia salina) bioassay and compared with the standard podophyllotoxin. The
- Reddy, M. Siva Nagi,Kumari, B. Sailaja,Babu, B. Hari
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p. 942 - 946
(2013/02/22)
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- NOVEL CHROMENE AND THIOCHROMENE CARBOXAMIDE DERIVATIVES, METHODS FOR PREPARING SAME AND THERAPEUTIC APPLICATIONS OF SAME
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The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.
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Page/Page column 38
(2008/06/13)
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- QUATERNARY SALT CCR2 ANTAGONISTS
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Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
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Page/Page column 75-77
(2008/06/13)
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- Quaternary salt CCR2 antagonists
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Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
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Page/Page column 81
(2008/06/13)
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- Chromene and Chroman 3-Carboxamides and Some Related Compounds as a New Class of Centrally Acting Agents
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A number of chromene-3-carboxamides (7), 3-Aminochromans (11) and 3-aminomethylchromans (9) have been synthesized.Chromene-3-carboxamides have been found to exhibit strong central muscle relaxant activity compared to mephesin.
- Gupta, R. C.,Pratap, Ram,Prasad, C. R.,Anand, Nitya
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p. 344 - 347
(2007/10/02)
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