Design, synthesis, and biological evaluation of new 1,4‐diarylazetidin‐2‐one derivatives (β‐lactams) as selective cyclooxygenase‐2 inhibitors
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DOI: 10.1002/ardp.201900293
Abstract: A new series of 1,4‐diarylazetidin‐2‐one derivatives (β‐lactams) were designed and synthesized to evaluate their biological activities as selective cyclooxygenase‐2 (COX‐2) inhibitors. In vitro COX‐1 and COX‐2 inhibition studies showed that all compounds were selective inhibitors… read more here.
Keywords: one derivatives; new diarylazetidin; selective cyclooxygenase; derivatives lactams ... See more keywords
Design, synthesis, molecular modeling, and antimicrobial potential of novel 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives as DNA gyrase inhibitors.
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DOI: 10.1002/ardp.202100266
Abstract: A series of 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives were designed using the molecular hybridization method, characterized using different spectroscopic techniques, and evaluated for their in vitro antimicrobial activity. Most of the target compounds demonstrated good to moderate antimicrobial… read more here.
Keywords: one derivatives; pyrazol imino; dna gyrase; indolin one ... See more keywords
Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1
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DOI: 10.1002/ardp.202200577
Abstract: Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecule inhibitors lack selectivity or suffer from low bioactivity. To address this limitation, a… read more here.
Keywords: design synthesis; derivatives potent; quinazolin one; selective inhibitors ... See more keywords
Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids.
Sign Up to like & getrecommendations! Published in 2022 at "Chirality"
DOI: 10.1002/chir.23501
Abstract: We previously demonstrated that natural product-inspired 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones derivatives delivered potent and selective PIM kinases inhibitors however with non-optimal ADME/PK properties and modest oral bioavailability. Herein, we describe a structure-based scaffold decoration and a stereoselective approach… read more here.
Keywords: synthesis dihydropyrrolo; dihydropyrrolo pyrazin; pyrazin one; synthesis ... See more keywords
Novel spiro[indene‐1,2′‐quinazolin]‐4′(3′H)‐one derivatives as potent anticonvulsant agents: One‐pot synthesis, in vivo biological evaluation, and molecular docking studies
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.23234
Abstract: A new series of spiro[indene‐1,2′‐quinazolin]‐4′(3′H)‐one derivatives 4a–m were synthesized via a one‐pot method and evaluated for anticonvulsant activities using pentylenetetrazole (PTZ) and maximal electroshock (MES)‐induced seizures. Obtained results demonstrated that these compounds have not anticonvulsant… read more here.
Keywords: spiro indene; compound; quinazolin one; indene quinazolin ... See more keywords
Screening and identification of 3‐aryl‐quinolin‐2‐one derivatives as antiviral agents against influenza A
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DOI: 10.1002/jmv.28327
Abstract: Quinolin‐2‐one represents an important and valuable chemical motif that possesses a wide variety of biological activities; however, the anti‐influenza activities of quinolin‐2‐one‐containing compounds were rarely reported. Herein, we describe the screening and identification of 3‐aryl‐quinolin‐2‐one… read more here.
Keywords: identification aryl; aryl quinolin; quinolin one; antiviral agents ... See more keywords
SYNTHESIS OF THIENO[2,3- b ]PYRIDINYL-4H-3,1-BENZOXAZIN-4 ONE DERIVATIVES
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DOI: 10.1007/6135
Abstract: How to Cite Vasilin, V. K.; Darma, M. S.; Stroganova, T. A.; Krapivin, G. D. Chem . Heterocycl . Compd . 201 0 , 46 , 1031. [ Khim. Geterotsikl. Soedin. 2010 , 1270.] For this… read more here.
Keywords: benzoxazin one; one derivatives; synthesis thieno; chemistry ... See more keywords
Design, synthesis, and bioevaluation of novel oxoindolin-2-one derivatives incorporating 1-benzyl-1H-1,2,3-triazole
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DOI: 10.1007/s00044-019-02488-1
Abstract: In our search for novel bioactive molecules, three series of indolin-2-one derivatives incorporating 1-benzyl-1H-1,2,3-triazole moiety were synthesized. The compounds were initially designed as acetylcholine esterase (AChE) inhibitors based on the structural feature of donepezil, a… read more here.
Keywords: benzyl triazole; ache; incorporating benzyl; one derivatives ... See more keywords
Physicochemical properties and antimicrobial activity of new spirocyclic thieno[2,3-d]pyrimidin-4(3H)-one derivatives
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DOI: 10.1007/s10593-017-2057-1
Abstract: A number of 6'-methylidene-2,3-dihydro-1H-spiro[pyridine-4,5'-thieno[2,3-d]pyrimidin]-4'(3'H)-one derivatives, obtained as major products of a domino reaction between 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidines and electron-deficient alkynes, were characterized for their acid-base properties and lipophilicity and evaluated for the antimicrobial activity against a number… read more here.
Keywords: one derivatives; thieno; pyrimidin one; antimicrobial activity ... See more keywords
Synthesis of 5-hydroxyfuran-2(5H)-one derivatives (microreview)
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DOI: 10.1007/s10593-018-2345-4
Abstract: In this microreview, we describe methods for the synthesis of 5-hydroxyfuran-2(5H)-one derivatives, which have been published over the last 5 years. The main routes for the preparation of 5-hydroxyfuran-2(5H)-one derivatives include transformations of 2-oxocarboxylic acids,… read more here.
Keywords: hydroxyfuran one; one derivatives; synthesis hydroxyfuran; derivatives microreview ... See more keywords
Design, synthesis and biological evaluation of 3,4-dihydronaphthalen-1(2H)-one derivatives as Bcl-2 inhibitors
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DOI: 10.1007/s11164-017-2972-x
Abstract: A series of new 3,4-dihydronaphthalen-1(2H)-one derivatives (6a–f) were designed, and synthesized by the Claisen–Schmidt condensation reaction. Their structures were characterized by NMR, FTIR, and MS spectroscopy. Their antitumor activities against human neoplastic cell lines Hela,… read more here.
Keywords: design synthesis; evaluation dihydronaphthalen; biological evaluation; one derivatives ... See more keywords