383130-54-9Relevant academic research and scientific papers
Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase
Ferrari, Stefania,Morandi, Federica,Motiejunas, Domantas,Nerini, Erika,Henrich, Stefan,Luciani, Rosaria,Venturelli, Alberto,Lazzari, Sandra,Calò, Samuele,Gupta, Shreedhara,Hannaert, Veronique,Michels, Paul A. M.,Wade, Rebecca C.,Costi, M. Paola
experimental part, p. 211 - 221 (2011/03/19)
Folate analogue inhibitors of Leishmania major pteridine reductase (PTR1) are potential antiparasitic drug candidates for combined therapy with dihydrofolate reductase (DHFR) inhibitors. To identify new molecules with specificity for PTR1, we carried out a virtual screening of the Available Chemicals Directory (ACD) database to select compounds that could interact with L. major PTR1 but not with human DHFR. Through two rounds of drug discovery, we successfully identified eighteen drug-like molecules with low micromolar affinities and high in vitro specificity profiles. Their efficacy against Leishmania species was studied in cultured cells of the promastigote stage, using the compounds both alone and in combination with 1 (pyrimethamine; 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine). Six compounds showed efficacy only in combination. In toxicity tests against human fibroblasts, several compounds showed low toxicity. One compound, 5c (riluzole; 6-(trifluoromethoxy)- 1,3-benzothiazol-2-ylamine), a known drug approved for CNS pathologies, was active in combination and is suitable for early preclinical evaluation of its potential for label extension as a PTR1 inhibitor and antiparasitic drug candidate.
Microwave-assisted synthesis of propesticides 1,3,4-thiadiazole aminophosphonates
Wan, Rong,Wang, Peng,Han, Fen,Wang, Yao,Zhang, Jianqiang
experimental part, p. 864 - 870 (2011/04/22)
A novel and easy synthetic route to diethyl (5-substituted phenyl-1,3,4-thiadiazol-2-ylamino) (substituted phenyl) methylphosphonates has been achieved by the reaction of substituted benzylidene-5-(substituted phenyl)-1,3,4-thiadiazol-2-amines and diethyl phosphite under microwave irradiation. These 1,3,4-thiadiazole aminophosphonates were identified by infrared, 1H NMR, and elemental analyses. The target compounds were obtained in better yields (71-89%) and shorter time (10min) than with conventional heating.
Microwave-assisted synthesis of 1,3,4-thiadiazole Schiff base derivatives
Hu, Jun,Sun, Jianguang,Zhou, Taoyu,Xu, Yanhua
experimental part, p. 442 - 443 (2011/11/06)
A rapid and efficient microwave-assisted synthesis method for the preparation of 1,3,4-thiadiazole Schiff base derivatives is described. These 1,3,4-thiadiazole Schiff bases (5a-h) were identified by IR, 1H NMR, elemental analyses. The target c
Synthesis and insecticidal activities of novel 1,3,4-thiadiazole 5-fluorouracil acetamides derivatives: An RNA interference insecticide
Wan, Rong,Zhang, Jian-Qiang,Han, Fen,Wang, Peng,Yu, Peng,He, Qiu
experimental part, p. 280 - 292 (2012/02/03)
A series of novel 1,3,4-thiadiazole 5-fluorouracil acetamides derivatives were designed and synthesized. Their structures were confirmed by infrared, 1H NMR spectroscopy, and elemental analysis. The insecticidal activities against Tetranychus cinnabarinus
Synthesis of 1,3,4-thiadiazole chrysanthemamide derivatives promoted by phenyldichlorophosphate catalysis
Yu, Peng,Wan, Rong,Wang, Peng,Zhang, Jiang-Qiang,He, Qiu
experimental part, p. 719 - 721 (2011/04/24)
A series of novel pro-pesticides with the activity of both 1,3,4-thiadiazole and chrysanthemic acid were synthesised using phenyldichlorophosphate catalysis. These 1,3,4-thiadiazole chrysanthemamides were identified by IR, 1H NMR and elemental
Microwave-assisted synthesis of 1,3,4-thiadiazole aroylurea derivatives
Han, Feng,Wan, Rong,Wang, Peng,Wang, Yao,Wang, Jintang
experimental part, p. 674 - 676 (2010/03/03)
A rapid and efficient microwave-assisted synthesis method for the preparation of 1-aroyl-3-(5-aryl-1,3,4-thiadiazol-2-yl)urea is described. These 1,3,4-thiadiazole aroylureas (5a-f) were identified by IR, 1H NMR, elemental analyses and N-[5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-ylcarbamoyl]-2, 6-difuorobenzamide was confirmed by single-crystal X-ray diffraction. The target compounds were prepared under microwave in a shorter reaction time compared with conventional heating methods.
One pot synthesis of 1,3,4-thiadiazole thiazolidinone derivatives
Wang, Peng,Wan, Rong,Han, Fen,Wang, Yao
experimental part, p. 671 - 673 (2010/03/24)
One pot synthesis of 2-(substitutedphenyl)-3-[5-(substitutedphenyl)-1,3,4- thiadiazol-2-yl]thiazolidin-4-one was developed by the reaction of 1,3,4-thiadiazole, substituted benzaldehyde and mercaptoacetic acid. These compounds were identified by IR,
Antihypertensive Thiadiazoles. 1. Synthesis of Some 2-Aryl-5-hydrazino-1,3,4-thiadiazoles with Vasodilator Activity
Turner, Stephen,Myers, Malcolm,Gadie, Brian,Nelson, Anthony J.,Pape, Robin,et al.
, p. 902 - 906 (2007/10/02)
Some 2-Aryl-5-hydrazino-1,3,4-thiadiazoles have been synthesized and screened for antihypertensive activity.In general, compounds with a 2-substituted phenyl ring had higher activity than their 3- or 4-substituted counterparts or those containing heteroar
