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Literature DB >> 19246128

Synthesis, antifungal activities and 3D-QSAR study of N-(5-substituted-1,3,4-thiadiazol-2-yl)cyclopropanecarboxamides.

Xing-Hai Liu¹, Yan-Xia Shi, Yi Ma, Chuan-Yu Zhang, Wei-Li Dong, Li Pan, Bao-Lei Wang, Bao-Ju Li, Zheng-Ming Li.

Abstract

A series of cyclopropanecarboxamide were prepared and tested for antifungal activity in vivo. The preliminary bioassays indicated that some compounds are comparable to the commercial fungicides. To further explore the comprehensive structure-activity relationship on the basis of fungicidal activity data, comparative molecular field analysis (CoMFA) was performed, and a statistically reliable model with good predictive power (r(2)=0.8, q(2)=0.516) was achieved. Based on the CoMFA, compound 7p was designed and synthesized, which was found to display a good antifungal activity (79.38%) as 7g and 7h.

Entities: Chemical

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Year: 2009 PMID： 19246128 DOI： 10.1016/j.ejmech.2009.01.012

Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514

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Cited

19 in total

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3. Green and four-component cyclocondensation synthesis and in silico docking of new polyfunctionalized pyrrole derivatives as the potential anticholinesterase agents.

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4. Synthesis and Antimicrobial Activity Screening of Piperazines Bearing N,N'-Bis(1,3,4-thiadiazole) Moiety as Probable Enoyl-ACP Reductase Inhibitors.

Authors: Alaa Z Omar; Najla A Alshaye; Tawfik M Mosa; Samir K El-Sadany; Ezzat A Hamed; Mohamed A El-Atawy
Journal: Molecules Date: 2022-06-09 Impact factor: 4.927

5. Synthesis of new chiral 1,3,4-thiadiazole-based di- and tri-arylsulfonamide residues and evaluation of in vitro anti-HIV activity and cytotoxicity.

Authors: Maria Shafique; Shahid Hameed; Muhammad Moazzam Naseer; Najim Aboud Al-Masoudi
Journal: Mol Divers Date: 2018-07-02 Impact factor: 2.943

Synthesis, antifungal activities and 3D-QSAR study of N-(5-substituted-1,3,4-thiadiazol-2-yl)cyclopropanecarboxamides.

1. Synthesis of some new pyrazolo[1,5-a]pyrimidine, pyrazolo[5,1-c]triazine, 1,3,4-thiadiazole and pyridine derivatives containing 1,2,3-triazole moiety.

2. Facile, efficient and one-pot access to diverse new functionalized aminoalkyl and amidoalkyl naphthol scaffolds via green multicomponent reaction using triethylammonium hydrogen sulfate ([Et₃NH][HSO₄]) as an acidic ionic liquid under solvent-free conditions.

3. Green and four-component cyclocondensation synthesis and in silico docking of new polyfunctionalized pyrrole derivatives as the potential anticholinesterase agents.

4. Synthesis and Antimicrobial Activity Screening of Piperazines Bearing N,N'-Bis(1,3,4-thiadiazole) Moiety as Probable Enoyl-ACP Reductase Inhibitors.

5. Synthesis of new chiral 1,3,4-thiadiazole-based di- and tri-arylsulfonamide residues and evaluation of in vitro anti-HIV activity and cytotoxicity.

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8. 2-Chloro-N-{5-[(4R,5R,10S)-dehydro-abiet-4-yl]-1,3,4-thia-diazol-2-yl}benzamide.

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10. (E)-(4-Bromo-benzyl-idene)amino cyclo-propane-carboxyl-ate.