- Synthesis and properties of diaminothiadiazoles
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Refined synthetic procedure for preparation of 3,5-diamino-1,2,4- thiadiazole and 2,5-diamino-1,3,4-thiadiazole based on the reaction of dithiourea or amidinothiourea with hydrogen peroxide is developed. The optimal reagents ratio was found, and monitoring methods were developed. It resulted in the increase of the target product yield and in a shorter reaction time. On the basis of 2,5-diamino-1,3,4-thiadiazole the alkylsubstituted 1,3,4- diaminothiadiazolidines were synthesized. The compounds prepared were characterized by the elemental analysis data, the IR, 1H NMR, and electronic spectra, and also by mass spectrometry.
- Melenchuk,Danilova,Stryapan,Islyaikin
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- Synthesis and biological activities on metal complexes of 2,5-diamino-1,3,4-thiadiazole derived from semicarbazide hydrochloride
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A bioactive ligand, 2,5-diamino-1,3,4-thiadiazole (L), derived from semicarbazide hydrochloride, and its metal complexes were prepared and characterized. The complexes were characterized using elemental, infra-red, ultraviolet/visible, magnetic moment, atomic absorption, thin layer chromatography and molar conductance measurements. The IR data revealed that the ligand (L) behaved as a tridentate neutral ligand. It coordinated to the metal ion via sulphur and nitrogen of the amines. The molar conductance data reveal that the chelates are non-electrolytes. From the Ultraviolet/Visible spectra and magnetic moment data, the complexes were found to have octahedral geometrical structure. In vivo evaluation of the antimicrobial activities of the metal complexes and the ligands showed greater activity against some micro-organisms when compared to the parent compounds. The chelates do not show toxicity against the activities of enzymes from homogenates of liver, kidney and serum in experimental rats.
- Obaleye, Joshua A.,Adediji, Johnson F.,Adebayo, Matthew A.
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- Synthesis and molecular docking of hybrids ionic azole Schiff bases as novel CDK1 inhibitors and anti-breast cancer agents: In vitro and in vivo study
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Three new hybrid ionic vanillyl-azole-Schiff bases (IVASBs) have synthesized and their antitumor performances were assessed in vitro against MCF-7 cells and in vivo against Ehrlich solid tumor (EST). The high binding energy score of IVASB3?CDK1 (?3.43 kca
- Abdelghany, Yasmin M.,Abdelhamid, Moustafa S.,Elshaarawy, Reda F. M.,Serag, Waleed M.,Zahran, Faten
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- Facile synthesis of novel bis-derivatives of 2,5-diamino-thiadiazole/N,N′-thiocarbohydrazide and their biological perspective
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A series of new bis derivatives of 2,5-thiadiazole and N,N′-thiocarbohydrazide along with their transition metal complexes were synthesized by green methods (sonochemical and microwave), i.e., energy and time efficient and operationally more simple than existing conventional methods. All the synthesized compounds were fully characterized by routine analytical techniques and subjected to a preliminary biological screening. These novel characterized compounds were screened for antimicrobial activities and showed promising results. A few potent compounds were also tested for antitumor activities against MDA-MB231 (human breast carcinoma cell line) and compound 5 has emerged as a potential antitumor compound followed by compound 2, 10 and 9, with IC50 values of 29.48, 32.25, 32.34 and 34.34?μg/ml, respectively. To understand the binding interactions of these compounds, in silico studies were performed using the AUTODOCK 4.2 suite and found to be supportive of the experimental results.
- Bhatt, Priyanka,Sreekanth,Jha, Anjali
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p. 7241 - 7258
(2018/09/06)
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- Composition of matter having bioactive properties
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Particles of coordinated complex comprising a basic, hydrous polymer and a capacitance adding compound, as well as methods for their production, are described. These complexes exhibit a high degree of bioactivity making them suitable for a broad range of applications through their incorporation into conventional vehicles benefiting from antimicrobial and similar properties.
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- Synthesis and anthelmintic activity of carbamates derived from imidazo[2,1-b][1,3,4]thiadiazole and imidazo[2,1-b]thiazole
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The anthelmintic activity of 25 compounds, most of them carbamates, was determined. The in vitro results are interesting and show that an aromatic azapentalene can replace the benzimidazole ring without loss of its biological properties. The in vivo resul
- Marin,Valls,Berenguer,Alonso,Martinez,Martinez,Elguero
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