New heterocyclic derivatives of cyclopropane dicarboxylic acid comprising thiadiazole and 1,2,4-triazole moieties are reported. Reaction of 1,1-cyclopropane dicarboxylic acid (1) with thiosemicarbazide and phosphorous oxychloride resulted in 1,1-bis (2-amino-1,3,4-thiadiazol-5- yl)cyclopropane (2). Cyclopropane dicarboxylic acid thiosemicarbazide (6) was converted into 1,1-bis(3-thio-4H-1,2,4-t...

The lipophilicity of two series of thiosemicarbazide derivatives was assessed by the RP-HPLC method with the RP-18 chromatographic column and the methanol-water mixture as the mobile phase. Distribution coefficients logPHPLC were compared to calculated values generated by commonly used AClogP software and quantum chemical calculations. The reliability of the predictions was evaluated using the ...

A series of heterocyclic compounds bearing the well-known free radical scavenging 3,4,5-trimethoxybenzyloxy group, was synthesized. The key compound 4-(3,4,5-trimethoxybenzyl-oxy)benzohydrazide was converted into thiosemicarbazide derivatives, which were subsequently cyclized with NaOH to provide 1,2,4-triazole derivatives. Alternative treatment of the acid hydrazide with carbon disulfide in th...

Utilization of benzoxazinone for synthesis quinazolinone derivatives with 3-heterocycle side chain. treatment of benzoxazinon 1 with cyano acetohydrazide or thionocarbohydrazide gave the quinazolinone derivatives 2 or 12. quinazolinone 2 has been utilized as synthon for new  pyridinone, oxazet, thiazole, thiazolidinone and quinazolinone derivatives. Thiosemicarbazide and thiosemicarbazone deriv...

Thiosemicarbazone and 4-thiazolidinone derivatives were synthesized in one and two step, respectively, from thiosemicarbazide, in satisfactory yields. Then, the synthesized compounds were submitted to evaluation against host cells infected with Toxoplasma gondii. The present studies showed that thiosemicarbazones 2 and 4-thiazolidinone derivatives 3 were effective against intracellular T. gondii.

a series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. the 4-amino-1,2,4-triazole-5-thione analogues (ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...