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Jilloju Parameshwara Chary Persoons Leentje Kurapati Sathish Kumar Schols Dominique De Jonghe Steven Daelemans Dirk Vedula Rajeswar Rao 《Molecular diversity》2022,26(3):1357-1371
A new series of (?±)-(3-(3,5-dimethyl-1H-pyrazol-1-yl)-6-phenyl-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-7-yl)(phenyl)methanones were efficiently synthesized starting from 4-amino-5-hydrazinyl-4H-1,2,4-triazole-3-thiol 1, acetyl acetone 2, various aromatic and heterocyclic aldehydes 3 and phenacyl bromides 4. All the newly synthesized compounds were tested for their antiviral and antitumoral activity. It was shown that subtle structural variations on the phenyl moiety allowed to tune biological properties toward antiviral or antitumoral activity. Mode-of-action studies revealed that the antitumoral activity was due to inhibition of tubulin polymerization.
Graphic abstract 相似文献2.
Parameshwara Chary Jilloju 《合成通讯》2018,48(14):1739-1746
A facile, one-pot three-component protocol for the synthesis of substituted 4-(benzylideneamino)-5-(3,5-dimethyl-1H-pyrazol-1-yl)-4H-1,2,4-triazole-3-thiols have been reported by the reaction of 4-amino-5-hydrazinyl-4H-1,2,4-triazole-3-thiol with acetyl acetone and various substituted benzaldehydes via multi component reaction. The newly synthesized derivatives were characterized by their elemental analysis and spectral data. The current strategy provides heterocyclic compounds in good yields with broad substrate scope. 相似文献
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Parameshwara Chary Jilloju Allam Vinaykumar Perugu Shyam Rajeswar Rao Vedula 《Journal of heterocyclic chemistry》2019,56(3):1012-1019
A facile and simple one‐pot procedure for the synthesis of various aralkyl/alkylthio‐3,5‐dimethyl‐1H‐pyrazolyl‐4H‐1,2,4‐triazol‐4‐amines has been described via a multicomponent reaction of 4‐amino‐5‐hydrazinyl‐4H‐1,2,4‐triazole‐3‐thiol, acetylacetone, and various aryl/alkyl halides in good yields. All the newly synthesized compounds were characterized by using analytical and spectral studies. Our in silico studies confirmed that 4e , 4f , 4g , and 4j have the best inhibition activity among the synthesized compounds with a high selective index against the Tubulin protein and showed best interactions with receptor structure. The present study provides a novel series of compounds with a promising inhibitor to prevent on Tubulin protein. 相似文献
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