scholarly journals Synthesis and Biological Evaluation of Novel Pyrane Glycosides

2020 ◽  
Vol 67 (4) ◽  
pp. 1061-1071
Author(s):  
Avula Srinivas ◽  
Malladi Sunitha ◽  
Sriramoju Shamili
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
Hydroxylamine Hydrochloride ◽  
Biological Evaluation ◽  
Chalcone Derivatives ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel (5R)-5-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-3-(4-fluorophenyl)-2,6-diphenyl-3,3a,5,6-tetrahydro-2H-pyrazolo[3,4-d]thiazoles 11a–g and (5R)-5-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-3-(4-fluorophenyl)-6-phenyl-3,3a,5,6-tetrahydroisoxazolo[3,4-d]thiazoles 12a–g were synthesized by the reaction of chalcone derivatives of (R,Z)-2-((2S,3S)-3-((1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-3,6-dihydro-2H-pyran-2-yl)-5-(4-fluorobenzylidene)-3-phenylthiazolidin-4-ones 10a–g with phenylhydrazine and hydroxylamine hydrochloride. The chemical structures of newly synthesized compounds were elucidated by IR, NMR, MS and elemental analysis. The compounds 11a–g and 12a–g were evaluated for their antibacterial activity and antifungal activity.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
Ic50 Values ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
H Nmr ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 ＞ 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2019 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
H Nmr ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

Synthesis and biological evaluation of chalcone derivatives of 1,2,4-thiadiazol-benzo[d]imidazol-2-yl)quinolin-2(1H)-one as anticancer agents

2020 ◽  
Vol 30 ◽  
pp. 100556
Author(s):  
Yazala Jyothsna Pragathi ◽  
Deekala Veronica ◽  
Kowthalam Anitha ◽  
Mandava Venkata Basaveswara Rao ◽  
Rudraraju Ramesh Raju
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Chalcone Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

scholarly journals Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole

2014 ◽  
Vol 79 (3) ◽  
pp. 277-282
Author(s):  
Vesna Vasic ◽  
Jelena Penjisevic ◽  
Irena Novakovic ◽  
Vladimir Sukalovic ◽  
Deana Andric ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antifungal Activity ◽  
Salmonella Enteritidis ◽  
Biological Evaluation ◽  
Proteus Vulgaris ◽  
Clostridium Sporogenes ◽  
In Vitro Antibacterial Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Series of eight novel 5-substituted derivatives of benzimidazole were synthesized by condensation of corresponding diamine with ethyl-4-[4-(2-chlorophenyl)piperazin-1-yl] butanoate in refluxing 4N hydrochloric acid. In vitro antibacterial activity against ten strains namely, Bacillus subtilis, Clostridium sporogenes, Streptosporangium longisporum, Micrococcus flavus, Sarcina lutea, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris and antifungal activity against two fungal strains namely, Candida albicans and Saccharomyces cerevisiae, were evaluated. Of all the compounds screened for activity 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-iodo-1H-benzimidazole and 2-{3-[4-(2-chlorophenyl)piperazin-1-yl]propyl}-5-methyl-1H-benzimidazole were associated with higher antifungal activity than commercial drugs.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
H Nmr ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 ＞ 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME HETEROCYCLES CONTAINING OXADIAZOLE AND PYRAZOLE RING FOR ANTI-BACTERIAL, ANTI-FUNGAL AND ANTI-TUBERCULAR ACTIVITIES

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 18-24
Author(s):  
S. R. Pattan ◽  
◽  
P. A Chavan ◽  
R. A Muluk ◽  
S. S Dengale ◽  
...  
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
Ethyl Acetoacetate ◽  
Pyrazole Ring ◽  
Biological Evaluation ◽  
Secondary Amines ◽  
Anti Fungal ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

1, 3, 4-oxadiazoles were synthesized by treating pyrazine-2-carbohydrazide with CS2 and alc. KOH and their derivatives were prepared by using R-Cl compounds. pyrazolones were synthesized by treatingpyrazine-2-carbohydrazide with ethyl acetoacetate. The derivatives of pyrazolone were prepared by refluxing pyrazolone with formaldehyde and different substituted secondary amines. All the synthesized compounds were characterized by IR, 1H-NMR and elemental analysis and evaluated for antibacterial, antifungal and antitubercular activities.

Synthesis and Biological Evaluation of Chalconyl Incorporated Schiff’s Bases of Sulphonamides

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Neeraj Kumar ◽  
Dhruti Bhatt ◽  
Chandra Shekhar Sharma ◽  
Hamendra Pratap Singh ◽  
Harshda Pandiya ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Biological Evaluation ◽  
Antibacterial And Antifungal Activity ◽  
Schiff’S Bases ◽  
E Coli ◽  
Schiff's Bases ◽  
Microbial Strains ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

A series of of Chalconyl Incorporated Schiff’s Bases of Sulphonamides was synthesized by reacting substituted chalcone derivatives with Sulphacetamide sodium in methanol. All the title compounds synthesized (2a-2d) were tested for antibacterial and antifungal activity using E. coli, P. aeruginosa, S. aureus, S. pyogenus and C. albicans, A. niger and A. clavatus respectively as microbial strains and Sulphacetamide sodium as standard. The compound 2d showed significant antibacterial activity and 2a showed moderate antifungal activity as compared with Sulphacetamide Sodium.

scholarly journals Synthesis and biological evaluation of novel urea and thiourea derivatives of valacyclovir

2014 ◽  
Vol 79 (3) ◽  
pp. 283-289 ◽  
Author(s):  
Ramana Katla ◽  
Rasheed Syed ◽  
Madhava Golla ◽  
Adam Shaik ◽  
Raju Chamarthi
Keyword(s):  
Antioxidant Activity ◽  
Antiviral Activity ◽  
Elemental Analysis ◽  
Antioxidant Activities ◽  
Biological Evaluation ◽  
Thiourea Derivatives ◽  
Mass Spectral ◽  
High Yields ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel urea and thiourea derivatives of valacyclovir were efficiently synthesized in high yields and evaluated their antiviral activity. 2-((6-Amino-4-oxo-4,5-dihydro-1H-imidazo[4,5-c]pyridin-1-yl)methoxy)ethyl-2-amino-3-ethylbutanoate (valacyclovir) 1 is reacted with various aromatic isocyanates/thiocyanates 2 in the presence of N, N- dimethyl piperazine as a base in THF: pyridine (4:1) to obtain valacyclovir urea/thiourea derivatives 3(a-j). The structures of the title compounds 3(a-j) were confirmed by IR, NMR (1H, 13C), mass spectral and elemental analysis. The newly synthesized compounds were screened for their antiviral activity against Tobacco mosaic virus (TMV) and antioxidant activity was evaluated by DPPH, SOD and GST methods. The title compounds exhibited potent antiviral and good antioxidant activities.

scholarly journals Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives

2008 ◽  
Vol 2008 ◽  
pp. 1-4 ◽  
Author(s):  
Ying Yang ◽  
Wen-Jun Mao ◽  
Huan-Qiu Li ◽  
Tao-Tao Zhu ◽  
Lei Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Line ◽  
Jurkat Cell ◽  
Preliminary Investigation ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Chemical Structures ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35×10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs) was also discussed based on the obtained experimental data.

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