614-10-8Relevant academic research and scientific papers
Diaryl-substituted thiosemicarbazone: A potent scaffold for the development of New Delhi metallo-β-lactamase-1 inhibitors
Li, Jia-Qi,Sun, Le-Yun,Jiang, Zhihui,Chen, Cheng,Gao, Han,Chigan, Jia-Zhu,Ding, Huan-Huan,Yang, Ke-Wu
, (2020/12/30)
The superbug infection caused by New Delhi metallo-β-lactamase (NDM-1) has become an emerging public health threat. Inhibition of NDM-1 has proven challenging due to its shuttling between pathogenic bacteria. A potent scaffold, diaryl-substituted thiosemicarbazone, was constructed and assayed with metallo-β-lactamases (MβLs). The obtained twenty-six molecules specifically inhibited NDM-1 with IC50 0.038–34.7 μM range (except 1e, 2e, and 3d), and 1c is the most potent inhibitor (IC50 = 0.038 μM). The structure-activity relationship of synthetic thiosemicarbazones revealed that the diaryl-substitutes, specifically 2-pyridine and 2-hydroxylbenzene improved inhibitory activities of the inhibitors. The thiosemicarbazones exhibited synergistic antimycobacterial actions against E. coli-NDM-1, resulted a 2–512-fold reduction in MIC of meropenem, while 1c restored 16–256-, 16-, and 2-fold activity of the antibiotic on clinical isolates ECs, K. pneumonia and P. aeruginosa harboring NDM-1, respectively. Also, mice experiments showed that 1c had a synergistic antibacterial ability with meropenem, reduced the bacterial load clinical isolate EC08 in the spleen and liver. This work provided a highly promising scaffold for the development of NDM-1 inhibitors.
Synthesis, characterization, and antioxidant activity of some new N 4-arylsubstituted-5-methoxyisatin-β-thiosemicarbazone derivatives
Mu?lu, Halit
, p. 2083 - 2098 (2020/01/13)
Abstract: Firstly, thiosemicarbazides were prepared by the reaction of hydrazine monohydrate with isothiocyanates in cold dry ethanol at 0?°C for 1?h. After that, new isatin-β-thiosemicarbazones were synthesized by treatment of 5-methoxyisatin with thiose
Isatin based thiosemicarbazide derivatives as potential inhibitor of α-glucosidase, synthesis and their molecular docking study
Hayat, Shawkat,Iqbal, Naveed,Khan, Khalid Mohammed,Nawaz, Muhammad,Qureshi, Faiza,Rab, Abdur,Rahim, Fazal,Shah, Syed Adnan Ali,Taha, Muhammad,Uddin, Imad,Uddin, Nizam,Wadood, Abdul,Zaman, Khalid
, (2020/07/25)
A new series of isatin based thiosemicarbazide derivatives 1–15 were synthesized and characterized by 1H NMR, 13C NMR and HR-EIMS. The synthetic derivatives were evaluated for α-glucosidase inhibitory potential. All compounds showed
Synthesis and fungicidal activities of some 2-substituted arylamino-5-(2′-furyl)-1,3,4-thiadiazolo[3,2-c]thiazoles and 5-substituted aryl-2-substituted arylamino-1,3,4-thiadiazolo[3,2-c]thiazoles
Tiwari, Shailendra,Nizamuddin
, p. 679 - 683 (2013/07/26)
Several 2-substituted arylamino-5-(2′-furyl)-1,3,4-thiadiazolo[3,2-c] thiazoles have been synthesised by cyclisation of 3-substituted aryl thiocarbanilido-2-(2′-furyl)thiazolidin-4-ones with cone. H 2SO4 with constant stirring in cold and 5-substituted aryl-2-substituted arylamino-1,3,4-thiadiazolo[3,2-c]thiazoles have been synthesised by the cyclisation of 2-substituted aryl-3-substituted arylthiourido-thiazolidin-4-ones with cone. H2SO4 with constant stirring in cold and screened for their antifungal activities against Helminthosporium oryzae and Cephalosporium sacchari.
Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors
Liu, Yang,Lu, Wei-Qiang,Cui, Kun-Qiang,Luo, Wei,Wang, Jian,Guo, Chun
, p. 1525 - 1531 (2013/03/14)
A series of novel artemisinin derivatives were synthesized from artemisinin and different anilines. All compounds were obtained as β-isomers. The target compounds were evaluated for inhibition activity against Plasmodium falciparum falcipain-2 in vitro, and most of them exhibited potent inhibition in the low micromolar range and proved to be new types of falcipain-2 inhibitors.
Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors
Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Tsu-An,Yueh, Andrew,Lee, Chung-Chi,Lee, Yen-Chun,Lee, Ching-Yin,Chao, Yu-Sheng,Shih, Shin-Ru,Chern, Jyh-Haur
scheme or table, p. 1948 - 1952 (2011/05/04)
A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.
Novel bis(thiosemicarbazones) of the 3,5-diacetyl-1,2,4-triazol series and their platinum(ii) complexes: chemistry, antiproliferative activity and preliminary nephrotoxicity studies
Matesanz, Ana I.,Hernandez, Carolina,Rodriguez, Ana,Souza, Pilar
experimental part, p. 5738 - 5745 (2011/08/04)
The preparation and characterization of three novel 4N- monosubstituted bis(thiosemicarbazone) ligands of 3,5-diacetyl-1,2,4-triazol series and their dinuclear platinum complexes are described. The crystal and molecular structure of the [Pt(μ-H
Synthesis and anticonvulsant evaluation of some novel (thio)semicarbazone derivatives of arylalkylimidazole
Calis, Uensal,Septioglu, Ebubekir,Aytemir, Mutlu Dilsiz
experimental part, p. 327 - 334 (2012/02/02)
A number of novel 2-(1H-imidazole-1-yl)-1-aryl-substituted ethane-1-one N-substituted phenyl(thio)semicarbazones (1-14) were synthesized to test for their anticonvulsant activity against the two seizure models, maximal electroshock (MES) and subcutaneous
Synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave
Shi, Zhi Chuan,Zhao, Zhi Gang,Liu, Xing Li,Chen, Yu
experimental part, p. 405 - 408 (2012/01/05)
An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed. Its main advantages are short reaction times, good conversions and the environmentally friendly nature of the process. The preliminary results indicate that some of these compounds possess inhibitory effects against E. coli.
Synthesis, anticonvulsant and toxicity screening of thiazolyl-thiadiazole derivatives
Siddiqui, Nadeem,Ahsan, Waquar
experimental part, p. 261 - 268 (2012/02/13)
Various thiazole-substituted thiadiazole derivatives (7a-t) were designed and synthesized using substituted acetophenones and substituted anilines as starting materials. Thiazole and thiadiazole moieties being anticonvulsants were clubbed together to get the titled compounds and their in vivo anticonvulsant screening were performed by two most adopted seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Three compounds 7i, 7l and 7n were found to be potent in both the screens with comparable ED50 and better TD50 values than some standard drugs. These compounds were also found to exert lesser toxic effects on liver.
