Crystal structure of 1-methoxy-5-methyl-N-phenyl-1,2,3-triazole-4-carboxamide

The title compound, C11H12N4O2,was prepared via the transformation of sodium 4-acetyl-1-phenyl-1H-[1.2.3]triazolate under the action of methoxyamine hydrochloride. The dihedral angle between the triazole and phenyl rings is 25.12 (16)° and the C atom of the methoxy group deviates from the triazole plane by 0.894 (4)Å. The conformation of the CONHR-group is consolodated by an intramolecular N—H...N hydrogen bond to an N-atom of the triazole ring, which closes an S(5) ring. In the crystal, weak N—H...N hydrogen bonds link the molecules into C(6) [010] chains

Zebrafish Models in NeuroPsychopharmacology and CNS Drug Discovery

Despite the high prevalence of neuropsychiatric disorders, their aetiology and molecular mechanisms remain poorly understood. The zebrafish (Danio rerio) is increasingly utilized as a powerful animal model in neuropharmacology research and in vivo drug screening. Collectively, this makes zebrafish a useful tool for drug discovery and the identification of disordered molecular pathways. Here, we discuss zebrafish models of selected human neuropsychiatric disorders and drug-induced phenotypes. As well as covering a broad range of brain disorders (from anxiety and psychoses to neurodegeneration), we also summarize recent developments in zebrafish genetics and small molecule screening, which markedly enhance the disease modelling and the discovery of novel drug targets

Synthesis and bioactivity of N-tert-butyl-N′-acyl-5-methyl-1,2,3- thiadiazole-4-carbohydrazides

A series of novel N-tert-butyl-N′-acyl-5-methyl-1,2,3-thiadiazole-4- carbohydrazides were designed and synthesized. Their structures were characterized by melting points, 1H NMR, IR, ESI-MS, and elemental analysis. The bioassay tests indicated that compound 7o exhibited excellent direct anti-TMV activity and induction activity in vivo at 50 μg/mL, which was better than that of Ninamycin and tiadinial. Our studies indicated that 1,2,3-thiadiazole was an active substructure for novel pesticide development. © 2012 Zhi Jin Fan. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved

A new ring transformation of 1,2,3-thiadiazoles into furan-2-carbothioamides

2-(5-Amino-1,2,3-thiadiazol-4-ylmethylene)malonates transform into furans containing thioamide groups

Zebrafish models in neuropsychopharmacology and CNS drug discovery

Despite the high prevalence of neuropsychiatric disorders, their aetiology and molecular mechanisms remain poorly understood. The zebrafish (Danio rerio) is increasingly utilized as a powerful animal model in neuropharmacology research and in vivo drug screening. Collectively, this makes zebrafish a useful tool for drug discovery and the identification of disordered molecular pathways. Here, we discuss zebrafish models of selected human neuropsychiatric disorders and drug-induced phenotypes. As well as covering a broad range of brain disorders (from anxiety and psychoses to neurodegeneration), we also summarize recent developments in zebrafish genetics and small molecule screening, which markedly enhance the disease modelling and the discovery of novel drug targets. © 2017 The British Pharmacological Societ