Synthesis and in vitro microbiological evaluation of an array of biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides

Kanagarajan, V.; Thanusu, J.; Gopalakrishnan, Mahesh

doi:10.1016/j.ejmech.2009.12.068

Cited by 48 publications

(26 citation statements)

References 23 publications

(20 reference statements)

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“…8,41.3,102.7,115.4,116.0,124.0 (q,JCF = 273.4 Hz),125.7 (q,JCF = 3.6 Hz),127.8,128.9,129.8,130.2 (q,JCF = 32.2 Hz),130.9,136.4,139.7,152.7,158.3,162.1,167.1,171.0 …”

Section: -(2-((3-cyano-6-phenyl-4-(4-(trifluoromethyl)phenyl)pyridinmentioning

confidence: 99%

“…cell proliferation and survival, invasion and metastasis, and angiogenesis. 8 Expression of ERK5 is significantly up-regulated in advanced prostate cancer and has been identified as an independent prognostic biomarker for aggressive disease. 9 ERK5 is over-expressed in 20% of breast cancer patients and its expression is an independent prognostic biomarker for reduced disease-free survival.…”

Section: Introductionmentioning

confidence: 99%

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High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

et al. 2016

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Myers, S. M. et al. (2016) High-throughput screening and hit validation of extracellular-related kinase 5 (ERK5) inhibitors. ACS Combinatorial Science, 18(8), pp. 444-455. (doi:10.1021/acscombsci.5b00155) This is the author's final accepted version.There may be differences between this version and the published version. You are advised to consult the publisher's version if you wish to cite from it. AbstractThe extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP Progressive Binding System, and used to identify hits from a library of 57,617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and re-assay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits.Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.

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“…8,41.3,102.7,115.4,116.0,124.0 (q,JCF = 273.4 Hz),125.7 (q,JCF = 3.6 Hz),127.8,128.9,129.8,130.2 (q,JCF = 32.2 Hz),130.9,136.4,139.7,152.7,158.3,162.1,167.1,171.0 …”

Section: -(2-((3-cyano-6-phenyl-4-(4-(trifluoromethyl)phenyl)pyridinmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

et al. 2016

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“…This moiety has also found applications in the field of engineering [7] and polymers [8]. The amides are known to possess valuable biological activities [9][10][11].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 3-[4-(2-furoyl)-1-piperazinyl]-N- (substituted)propanamides as promising antibacterial agents with mild cytotoxicity

et al. 2018

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Purpose: To evaluate the antibacterial activity and cytotoxicity of a series of molecules with amalgamation of furoyl, piperazine and amide moieties. Methods: New derivatives, namely 3-[4-(2-furoyl)-1-piperazinyl]-N-(substituted)propanamides, were synthesized and evaluated for their antibacterial activity and toxicity to mammalian cells. The synthesis was initiated by treating different aryl/aralkyl amines (1a-u) with 3-bromopropionyl chloride (2) to obtain the solid electrophiles 3a-u, which were collected by filtration. Thereafter, and 2-furoyl-1-piperazine (4) at equimolar ratios were allowed to react in acetonitrile and in the presence of a base, K2CO3, to form the target compounds, 5a-u. Structural elucidation was carried out using EI-MS (electron impact mass spectrometry), IR (infrared) and 1H-NMR (proton nuclear magnetic resonance). The antibacterial activity of the synthesized compounds was evaluated against various bacterial strains. Furthermore, hemolysis was determined to assess cytotoxicity using bovine red blood cells. Results: Molecules 5g, 5a, 5p, 5g and 5i were found to be potent agents against S. aureus, S. typhi, P. 8.34 ± 0.55, 8.37 ± 0.12, 8.65 ± 0.57, 8.97 ± 0.12 and 9.24 ± 0.50 µM, compared to 7.80 ± 0.19, 7.45 ± 0.58, 7.14 ± 0.58, 7.16 ± 0.58 and 7.29 ± 0.90 aeruginosa, E. coli and B. subtilis with respective minimum inhibitory concentration (MIC) values of

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“…Hybrid 1,2,4-triazole and 1,3,4-oxadiazole compounds are new classes of azole anti-mycobacterials, which are proved to be highly active both in vitro and in vivo 11 . Schiff bases obtained from various heterocycles have a wide range of biological activities including antifungal, antibacterial, antimalarial, antimycobacterial, antimicrobial, anti-inflammatory, antiviral, cytotoxic, anticonvulsant, antiproliferative, anticancer, and antipyretic activities [12][13][14][15][16][17][18] . N-fuctionalized morpholines have diverse pharmacological activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities

Ünver

Deniz

Çelik

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Compound 2 was synthesized by reacting CS 2 /KOH with compound 1. The treatment of compound 2 with hydrazine hydrate produced compound 3. Then, compound 3 was converted to Schiff bases (4a-d) by the handling with several aromatic aldehydes. The treatment of triazole compounds 4a-d containing Schiff base with morpholine gave compounds 5a-d. All compounds were tested for their antioxidant and antimicrobial activities. The antioxidant test results of DPPH radical scavenging and ferric reducing/antioxidant power methods showed good antioxidant activity. The triazole-thiol (3) was the most active, and the effect of the substituent type of the thiophene ring on the activity was same for both Schiff bases (4a-d) and Mannich bases (5a-d). Among the newly synthesized triazole derivatives, the Schiff base 4d and the Mannich base 5d carrying nitro substituent on the thiophene ring showed promising antibacterial and antifungal activity, with lower MIC values than the standard antibacterial ampicillin.

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Synthesis and in vitro microbiological evaluation of an array of biolabile 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides

Cited by 48 publications

References 23 publications

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

Synthesis of 3-[4-(2-furoyl)-1-piperazinyl]-N- (substituted)propanamides as promising antibacterial agents with mild cytotoxicity

Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities

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