- 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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- 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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- ALLOSTERIC INHIBITORS OF ATYPICAL PROTEIN KINASES C
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The invention provides specific small molecule compounds that allosterically regulate the activity of atypical protein kinase C, their use as a medicament, and their use in the treatment and prevention of allergic, inflammatory and autoimmune disorders, cancer, hyperproliferation, sepsis, viral and protozoan infections, dementing diseases, metabolic, sclerotic and osteoporotic disorders.
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Paragraph 0090; 0108; 0140
(2015/06/08)
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- Discovery and optimization of 1,3,5-trisubstituted pyrazolines as potent and highly selective allosteric inhibitors of protein kinase C-χ
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There is increasing evidence that the atypical protein kinase C, PKCχ, might be a therapeutic target in pulmonary and hepatic inflammatory diseases. However, targeting the highly conserved ATP-binding pocket in the catalytic domain held little promise to
- Abdel-Halim, Mohammad,Diesel, Britta,Kiemer, Alexandra K.,Abadi, Ashraf H.,Hartmann, Rolf W.,Engel, Matthias
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supporting information
p. 6513 - 6530
(2014/10/15)
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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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- 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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