scholarly journals Fruit juice mediated multicomponent reaction for the synthesis of substituted isoxazoles and their in vitro bio-evaluation

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Susheel Gulati ◽  
Rajvir Singh ◽  
Suman Sangwan
Keyword(s):  
Raphanus Sativus ◽  
Cocos Nucifera ◽  
Hydroxylamine Hydrochloride ◽  
Erwinia Carotovora ◽  
Inhibition Zone ◽  
Herbicidal Activity ◽  
Xanthomonas Citri ◽  
One Pot ◽  
Three Component Reaction

AbstractA simple, efficient and eco-friendly procedure for the synthesis of isoxazole derivatives (4a–4h) using one-pot three-component reaction between substituted aldehydes (1a), methyl acetoacetate (2a) and hydroxylamine hydrochloride (3a) has been achieved in presence of Cocos nucifera L. juice, Solanum lycopersicum L. juice and Citrus limetta juice respectively. The homogeneity of synthesized compounds was confirmed by melting point and thin layer chromatography. The synthesized compounds were characterized by using 1H NMR, FTIR and CHN analyses and evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). The compounds (4a–4h) were also screened for their fungicidal activity against Rhizoctonia solani and Colletotrichum gloeosporioides. Antibacterial activity was also tested against Erwinia carotovora and Xanthomonas citri. From bio-evaluation data, it was found that compound 4b was most active against Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compound 4b was also found most active against both the fungus viz. R. solani and C. gloeosporioides showing maximum percentage growth inhibition i.e. 90.00 against R. solani and 82.45 against C. gloeosporioides at 2000 µg/mL concentration. Compound 4 h has shown maximum inhibition zone i.e. 3.00–9.60 mm against Erwinia carotovora at 2000 µg/mL concentration. Maximum Xanthomonas citri growth was also inhibited by compound 4 h showing inhibition zone 1.00–5.00 mm at highest concentration.

scholarly journals Fruit juice mediated multicomponent reaction for the synthesis of substituted isoxazoles and their in vitro bio evaluation

2021 ◽  
Author(s):  
Susheel Gulati ◽  
Rajvir Singh ◽  
Suman Sangwan
Keyword(s):  
Multicomponent Reaction ◽  
Raphanus Sativus ◽  
Cocos Nucifera ◽  
Erwinia Carotovora ◽  
Inhibition Zone ◽  
Herbicidal Activity ◽  
Xanthomonas Citri ◽  
Zone Method ◽  
One Pot

Abstract Abstract A simple, efficient and eco-friendly procedure for the synthesis of isoxazoles derivatives (4a-4h) using one-pot three components reaction between substituted aldehydes (1a), methyl acetoacetate (2a) and hydroxylamine hydrochloride (3a) has been achieved in presence of Cocos nucifera L. juice, Solanum lycopersicum L. juice and Citrus limetta juice respectively. This protocol is natural acid catalysed multicomponent reaction for the synthesis of potentially bioactive isoxazole derivatives. The homogeneity of synthesized compounds was confirmed by melting point and thin layer chromatography. The synthesized compounds were characterized by using 1HNMR, FTIR and CHN spectral analysis and evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). The compounds (4a-4h) were also screened for their fungicidal activity against Rhizoctonia solani and Colletotrichum gloeosporioides by poisoned food techniques. Antibacterial activity was also tested against Erwinia carotovora and Xanthomonas citri by inhibition zone method. From bio evaluation data, it was found that compound 4b was most active against Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compound 4b was also found most active against both the fungus viz. R. solani and C. gloeosporioides showing maximum percentage growth inhibition i.e. 90.00 against R. solani and 82.45 against C. gloeosporioides at 2000 µg/mL concentration. Compound 4h has shown maximum inhibition zone i.e. 3.00-9.60 mm against Erwinia carotovora at 2000 µg/mL concentration. Maximum Xanthomonas citri growth was also inhibited by compound 4h showing inhibition zone 1.00–5.00 mm at highest concentration. Less reaction time, high yields of desired products, mild reaction conditions, simple work-up, cost effectiveness and no need of column chromatography are some beauties of present methodology.

scholarly journals Fruit juice mediated multicomponent reaction for the synthesis of substituted isoxazoles and their in vitro bio evaluation

2021 ◽  
Author(s):  
Susheel Gulati Shelu ◽  
Rajvir Singh Rajvir ◽  
Suman Sangwan Suman
Keyword(s):  
Multicomponent Reaction ◽  
Raphanus Sativus ◽  
Cocos Nucifera ◽  
Erwinia Carotovora ◽  
Inhibition Zone ◽  
Herbicidal Activity ◽  
Xanthomonas Citri ◽  
Zone Method ◽  
One Pot

Abstract A simple, efficient and eco-friendly procedure for the synthesis of isoxazoles derivatives (4a-4h) using one-pot three components reaction between substituted aldehydes (1a), methyl acetoacetate (2a) and hydroxylamine hydrochloride (3a) has been achieved in presence of Cocos nucifera L. juice, Solanum lycopersicum L. juice and Citrus limetta juice respectively. This protocol is natural acid catalysed multicomponent reaction for the synthesis of potentially bioactive isoxazole derivatives. The homogeneity of synthesized compounds was confirmed by melting point and thin layer chromatography. The synthesized compounds were characterized by using 1HNMR, FTIR and CHN spectral analysis and evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). The compounds (4a-4h) were also screened for their fungicidal activity against Rhizoctonia solani and Colletotrichum gloeosporioides by poisoned food techniques. Antibacterial activity was also tested against Erwinia carotovora and Xanthomonas citri by inhibition zone method. From bio evaluation data, it was found that compound 4b was most active against Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compound 4b was also found most active against both the fungus viz. R. solani and C. gloeosporioides showing maximum percentage growth inhibition i.e. 90.00 against R. solani and 82.45 against C. gloeosporioides at 2000 µg/mL concentration. Compound 4h has shown maximum inhibition zone i.e. 3.00-9.60 mm against Erwinia carotovora at 2000 µg/mL concentration. Maximum Xanthomonas citri growth was also inhibited by compound 4h showing inhibition zone 1.00-5.00 mm at highest concentration. Less reaction time, high yields of desired products, mild reaction conditions, simple work-up, cost effectiveness and no need of column chromatography are some beauties of present methodology.

scholarly journals Fruit juices acts as biocatalyst in efficient synthesis of potentially bioactive imidazoles

2021 ◽  
Author(s):  
Susheel Gulati ◽  
Rajvir Singh ◽  
Suman Sangwan
Keyword(s):  
Rhizoctonia Solani ◽  
Raphanus Sativus ◽  
Colletotrichum Gloeosporioides ◽  
Cocos Nucifera ◽  
Inhibition Zone ◽  
Herbicidal Activity ◽  
Citrus Limon ◽  
Zone Method ◽  
Activity Data

Abstract An efficient and eco-friendly itinerary for the synthesis of imidazole derivatives (3a-3h) from reaction between substituted aldehydes (1a-1h), benzil (2a) and ammonium acetate (2b) in presence of Citrus limon L. juice, Vitis vinifera L. juice and Cocos nucifera L. juice has been carried out. The purity of compounds was confirmed by melting point and thin layer chromatography. All synthesized compounds (3a-3h) were characterized by 1HNMR, FTIR and CHN spectral techniques and tested for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). The compounds (3a-3h) were also evaluated for their antifungal activity against Rhizoctonia solani and Colletotrichum gloeosporioides by poisoned food techniques method. Antibacterial activity was also determined against Erwinia cartovora and Xanthomonas citri by inhibition zone method. From activity data, it was observed that compounds 3f and 3c were found most active against Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compound 3d was found most active against Rhizoctonia solani and Colletotrichum gloeosporioides fungus at highest concentration. Compound 3b has shown maximum inhibition zone i.e. 2.10-7.10 mm against Erwinia cartovora at 2000 µg/mL concentration. Maximum Xanthomonas citrii growth was inhibited by compounds 3c showing inhibition zone 1.00-5.00 mm at highest concentration.

Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
High Yield ◽  
Breast Cancer Cell Lines ◽  
Pyridine Derivatives ◽  
One Pot ◽  
Standard Drug ◽  
Three Component Reaction ◽  
Anti Cancer

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

scholarly journals Efficient and facile synthesis of pyrazoles using Guar-gum as biocatalyst and their in vitro bio-evaluation

2021 ◽  
Author(s):  
Suman Sangwan ◽  
Rajvir Singh ◽  
SUSHEEL GULATI ◽  
Suprita Rana
Keyword(s):  
Aspergillus Niger ◽  
Rhizoctonia Solani ◽  
Raphanus Sativus ◽  
Guar Gum ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Herbicidal Activity ◽  
Facile Synthesis ◽  
Solvent Free Conditions

Abstract A green efficient and facile synthesis of pyrazoles is reported via condensation reaction between substituted aldehydes (1a-1i), malononitrile (2) and 2,4-dinitrophenyl hydrazine (3) in presence of acylated Guar-gum as biocatalyst under solvent-free conditions. The progress of reaction was checked by thin layer chromatography and melting points reported are uncorrected. All synthesized compounds (4a-4i) were characterized by using 1HNMR and FTIR spectral techniques and evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). All compounds (4a-4i) were also evaluated for their antifungal activity against Rhizoctonia solani and Aspergillus niger by poisoned food techniques method. Antioxidant activity of synthesized compound was also determined. From activity results, it was found that compound 4f was most active against both Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compounds 4e and 4h were found most active against Rhizoctonia solani and Aspergillus niger fungus respectively at highest concentration. Compound 4e has shown maximum percentage DPPH free radical scavenging activity 1.e. 61.47% at 100 µg/mL concentration. Less reaction time, excellent yield of products, mild reaction conditions and simple work-up are some merits of present methodology.

Sulfated Tin Oxide: A Convenient Heterogeneous Catalyst for the Synthesis of 4-Arylmethylidene-3-substituted-isoxazol-5(4H)-ones

2021 ◽  
Vol 18 ◽  
Author(s):  
Nitishkumar S. Kaminwar ◽  
Sunil U. Tekale ◽  
Srinivas L. Nakkalwar ◽  
Rajendra P. Pawar
Keyword(s):  
Heterogeneous Catalyst ◽  
Tin Oxide ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Hydroxylamine Hydrochloride ◽  
One Pot ◽  
Easy Method ◽  
Three Component Reaction ◽  
Wide Range ◽  
The One

: Synthesis of isoxazole structural heterocyclic compounds is important due to their wide range of biological activities. In the present article, we report a convenient and easy method for the synthesis of 4-arylmethylidene-3-substituted-isoxazol-5(4H)-ones by the one-pot three-component reaction of aldehydes, β-keto ester, and hydroxylamine hydrochloride cat-alyzed by sulfated tin oxide as a heterogeneous catalyst.

PTSA-Catalyzed One Pot Domino Synthesis of Dihydropyrido[2,3-d]pyrimidine Derivatives and their Antimicrobial Activity

2021 ◽  
Vol 6 (3) ◽  
pp. 222-227
Author(s):  
Krishna A. Bhensdadia ◽  
Prakash L. Kalavadiya ◽  
Nilam H. Lalavani ◽  
Shipra H. Baluja
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Pyrimidine Derivatives ◽  
One Pot ◽  
In Vitro Antimicrobial Activity ◽  
Aryl Aldehydes ◽  
Three Component Reaction ◽  
The One

A novel series of dihydropyrido[2,3-d]pyrimidine derivatives were synthesized by multicomponent domino cyclization via the one-pot three component reaction of 6-amino uracil, substituted aryl aldehydes and N-methyl-1-(methylthio)-2-nitroethenamine in the presence of PTSA 10 mol% as a catalyst. The structures of these synthesized compounds were characterized by spectral analysis. Further the synthesized compounds screened for in vitro antimicrobial activity. Among all the compounds, compound 4b containing flouro substitution exhibited good inhibition against the tested species.

scholarly journals An Efficient, Three-Component Synthesis of Isoindolin-1-One-3-Phosphonates Under Mild and Solvent-Free Conditions and Their Biological Activities

2021 ◽  
Author(s):  
Hamida Jelali ◽  
Ibrahim S. Al Nasr ◽  
Waleed S. Koko ◽  
Tariq A. Khan ◽  
Eric Deniau ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Human Cancer ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Primary Amines ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
Solvent Free Conditions ◽  
Three Component Reaction

Abstract In this work, the synthesis of isoindolin-1-one-3-phosphonates by a ‘one-pot’ three-component reaction of 2-formylbenzoic acid with primary amines and dimethyl phosphite under solvent and catalyst free-conditions was reported. 1H NMR, 13C NMR, FT-IR and elemental analysis techniques, characterized the obtained compounds. The isoindolin-1-one-3-phosphonates were screened for their antimicrobial activities against bacteria and a fungus (Candida albicans). They were additionally also investigated for their anti-parasitical activities against Leishmania major promastigotes and amastigotes and Toxoplasma gondii in vitro. Cytotoxicity investigations of the isoindolin-1-one-3-phosphonates were led conducted in two human cancer cell lines, MDA-MB-231 and MCF-7and vero cells.

scholarly journals In Vitro Antifungal Efficacy of White Radish (Raphanus sativus L.) Root Extract and Application as a Natural Preservative in Sponge Cake

Processes ◽  
2019 ◽  
Vol 7 (9) ◽  
pp. 549
Author(s):  
Huynh Hoang Duy ◽  
Pham Thi Kim Ngoc ◽  
Le Thi Hong Anh ◽  
Dong Thi Anh Dao ◽  
Duy Chinh Nguyen ◽  
...  
Keyword(s):  
Raphanus Sativus ◽  
Ethanolic Extract ◽  
Inhibition Zone ◽  
Fungal Species ◽  
Root Extract ◽  
Sponge Cake ◽  
Radish Root ◽  
Raphanus Sativus L ◽  
White Radish

The study attempts the optimization of the total flavonoid content (TFC) and the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) antioxidant activity of the white radish (Raphanus sativus L.) root ethanolic extract (WRE) with regard to several parameters including ethanol concentration, the ratio of solvent/material, temperature and extraction time. Then antifungal analysis of WRE was performed against four fungal species including Aspergillus flavus NBRC 33021, Aspergillus niger NBRC 4066, Aspergillus clavatus NBRC 33020, and Fusarium solani NBRC 31094. At the WRE concentration of 75 mg/mL, diameters of inhibition zone were 9.11 ± 1.5, 19.55 ± 1.68, 17.72 ± 0.25, and 17.50 ± 0.73 mm respectively against the four examined species. Minimum fungal concentration (MFC) values of WRE against the four species were 30, 10, 20 and 30 mg/mL respectively. Evaluation of the sponge cake added with white radish root extract suggested that shelf-life of the sponge cake is 8 weeks in air-cooled condition (20 °C) and two weeks in warm condition (37 °C).

Sign in / Sign up

Export Citation Format

Share Document