Triazolo[3,4-b][1,3,4]thiadiazole molecules are found to be important tools in modern bioorganic and medicinal chemistry. This condensed system successfully combines two pharmacologically significant five-membered heterocycles – 1,2,4-triazole and 1,3,4-thiadiazole, which causes much more interest in the enhanced activity profile of its analogs than their parent separate constituents. It’s considered that the triazoles fused to thiadiazoles exhibit various therapeutically important properties, probably due to the existence of N-C-S fragments in their structures. In this review, we presented the summarized literature data about the diversity of pharmacological effects of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole based compounds as promising objects for the rational design of drug-like molecules.

This work includes the synthesis of ten heterocyclic compounds (3a-i and 4) containing pyrimidine moiety incorporated in their structures. Structure characterizations of these compounds were performed by using elemental and spectroscopic analyses. Their toxicity as potential insecticidal agents against the adults and nymphs of cowpea Aphid, Aphis craccivora Koch was evaluated. The results of this toxicological activity test revealed that a reasonable number of these compounds possess excellent toxicological activity against cowpea aphids such as compounds (3d), (3c), and (3b) with LC50 values 0.0125, 0.0134, and 0.0383 ppm, respectively. The toxicological activities of the rest of the tested compounds ranged from good to moderate against the same insects.

The present paper elicits the zinc oxide nanoparticles-assisted synthesis of a new series of seven-membered 1,4-diazepine heterocyclic compounds as potent lead scaffolds. Structures of synthesized compounds were corroborated using spectroanalytical techniques viz, FT-IR, 1H, 13C NMR, Mass, and elemental analysis. Also, Field emission scanning electron microscopy (FE-SEM), Transmission electron microscopy (TEM), Energy dispersive x-ray analysis (EDAX), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FT-IR) were used to establish the structure and morphology of the synthesized nanocatalyst. The clean workup procedure, high to excellent yields, relatively short reaction times, and high atom economy are the incredible advantages associated with the protocol.

Kinetic studies were made of the reactions between triphenylphosphine 1 and dialkyl acetylenedicarboxylates 2, in the presence of NH-acids, such as benzotriazole, 5-methylbenzotriazole or 5-chlorobenzotriazole 3 (as a protic/nucleophilic reagent). To determine the kinetic parameters of the reactions, they were monitored by UV spectrophotometry. Useful information was obtained from studies of the effect of solvent, structure of reactants (dialkyl acetylenedicarboxylates and NH-acids) and also concentration of reactants on the reaction rates. First and third steps (k2, k3) of all reactions were recognized as a rate determining and fast steps, respectively. Proposed mechanism was confirmed on the basis of experimental data.