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A 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. [ABSTRACT FROM AUTHOR]

New and facile one-pot three component approach for the synthesis of substituted dihydropyrimidinones derivatives (4a-4h) from reaction of equimolar substituted aldehydes (1a-1h), methyl acetoacetate (2a) and urea (3a) in presence of nature derived catalyst viz. Cocos nucifera L. juice, Solanum lycopersicum L. juice and Citrus limetta juice, commonly known as coconut juice, tomato juice and musambi juice respectively, at room temperature has been carried out. All synthesized compounds were evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish seeds). The compounds (4a-4h) were also screened for their antifungal activity against Rhizoctonia solani and Colletotrichum gloeosporioides by poisoned food techniques method. Antibacterial activity was also studied against Erwinia cartovora and Xanthomonas citri by inhibition zone method. From activity data, it was found that compounds 4g and 4d were most active against Raphanus sativus L. (root) and Raphanus sativus L. (shoot) respectively. Compounds 4f and 4c was found most active against Rhizoctonia solani and Colletotrichum gloeosporioides fungus respectively at highest concentration. Compound 4g has shown maximum inhibition zone i.e. 1.00–5.50 mm against Erwinia cartovora at 2000 μg/mL concentration. Maximum Xanthomonas citrii growth was inhibited by compounds 4f showing inhibition zone 4.00–12.00 mm at highest concentration. Short reaction time, high yields, mild reaction condition and simple work-up are some merits of present methodology. [ABSTRACT FROM AUTHOR]

An efficient and facile synthesis of substituted novel benzimidazoles (3a–3h) mediated by fruit juices viz. Cocos nucifera L. juice, Citrus limetta juice and Citrus sinensis L. juice, via condensation of substituted aldehydes (1a–1h) and o-phenylenediammine (2a) under solvent-free condition at room temperature is presented in this paper. The purity of compounds was confirmed by melting point and thin layer chromatography. All synthesized compounds (3a–3h) were fully characterized via NMR and FTIR spectral data and evaluated for in vitro herbicidal activity against Raphanus sativus L. (Radish) seeds. The compounds (3a–3h) were also evaluated for their antibacterial activity against Erwinia cartovora and Xanthomonas citri by inhibition zone method. Antifungal activity was also determined against Rhizoctonia solani and Colletotrichum gloeosporioides by poisoned food techniques method. From activity data, it was found that compounds 3d and 3e were most active against R. sativus L. (root) and R. sativus L. (shoot), respectively. Compound 3g has shown maximum inhibition zone i.e. 8.00 mm against E. cartovora at 2000 µg/mL concentration. Maximum X. citrii growth was inhibited by compounds 3a showing inhibition zone 5.20 mm at highest concentration. Compound 3f was found most active against R. solani and C. gloeosporioides fungus at 2000 µg/mL concentration. In comparison with the conventional methods, the present method complies with several key requirements of green chemistry principles such as the utilization of renewable feedstock, auxiliary aqueous conditions and reduces waste with the use of nature-derived catalyst. Therefore, the present method offers an attractive option because of its ecological safety, environmental acceptance, cost effective and easy workup process. [ABSTRACT FROM AUTHOR]