Synthesis and primary cytotoxicity evaluation of 3-[[(3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-1H-2-indolinones

Synthesis, Biological Evaluation of 1,3,4-Oxadiazole, Triazole and Uracil Derivatives from Poly (ethylene terephthalate) Waste

“…Treatment of the mercaptotriazole (10) with aromatic carboxylic acids, in the presence of POCl 3 in a one pot reaction, afforded [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazol-3-yl)benzoic acid derivatives (11a, b) yield ≈65-77% (Scheme 3). The structures of the latter products were assigned on the basis of their analytical and spectral data.…”

“…Moreover, compound 9 bearing substituted 1,3,4-oxadiazole moiety emerged as the most active member against Gram positive S. peneumoniae among its acid analogous in this study. On the other hand, incorporation of fused system [1,2,4] triazolo [3,4- [1,3,4]thiadiazole with the benzoic acid core led to compounds 11a and 11b, respectively. Compound 11a (18±0.043 mg/ml -1 ) was more potent than 11b against all tested Gram positive and Gram negative bacteria, whereas 11b showed superior antifungal activity against C. albicans than 11a.…”

“…Uracils, 1,3,4-oxadiazoles, 1,3,4-triazoles, and thiadiazoles were associated with diverse pharmacological activities as anti-mycobacterial (1) , antidiabetic agents (2) , kinase and phosphodiestrase inhibitors (3) , and for their valuable antiangiogenic (4) , fungicidal, cytotoxic antitubercular (5) , antimicrobial (6) and anthelmintic activities (7) . In this context, we report on the synthesis of uracil,1,3,4-oxadiazole, 1,3,4-triazole, and thiadiazole derivatives starting from dibutylterephthalate (2a) and 4-(butoxycarbonyl) benzoic acid (2b) which are obtained from degradation of PET bottle waste.…”

Crystal structure of 5-methoxy-N′-[(3Z)-5-chloro-1-(4-fluorobenzyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-1H-indole-2-carbohydrazide-DMSO (1/1), C25H18ClFN4O3 · C2H6OS

“…Therefore, indoles are privileged structures and it has been suggested that they are probably considered the most important of all structural classes in drug discovery [1][2][3]. On the other hand, the isatin (1H-indol-2,3-dione) moiety is the scaffold of many synthetically versatile molecules characterized by broad spectrum of biological activities [4][5][6][7]. The title molecule incorporats both indole and isatin moieties.…”

Design, Synthesis and Characterization of Novel Amine Derivatives of 5-[5-(Chloromethyl)-1, 3, 4-Oxadiazol-2-yl]- 2-(4-Fluorophenyl)-Pyridine as a New Class of Anticancer Agents

“…It was envisaged that the novel amine derivatives of 1, 3, 4-oxadiazole (Figure 1, B) would enhance the solubility, total polar surface area (TPSA) and bioavailability. With this view the compounds have been subjected to MTT assay 10 for testing their cytotoxic activity using 5-fluorouracil as the standard drug. Three human carcinoma cell lines were employed for the screening and the activity was calculated in terms of the IC 50 values.…”