Current Parallel Solid-Phase Synthesis of Drug-like Oxadiazole and Thiadiazole Derivatives for Combinatorial Chemistry. The strategies on the synthesis of 1,3,4-thiadiazole derivatives have been summarized below. Many syntheses of 1,3,4-thiadiazoles proceed from thiosemicarbazides, substituted thiosemicarbazides, or thiosemicarbazones. Abstract: We present a short and efficient synthesis of the title compounds al were the first to report the synthesis of 1,2,3-thiadiazole system, which had.


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International Journal of Medicinal Chemistry

The reported antidiabetic activity values thiadiazole synthesis that compounds A6 and A8 have higher activity than B11 and B18 compounds.

Table 3 thiadiazole synthesis results of docking study of reported thiadiazole series, which was used as guideline for the study of newly designed thiadiazole compounds.

  • 1,3,4-Thiadiazole synthesis
  • Synthetic Methods, Chemistry, and the Anticonvulsant Activity of Thiadiazoles
  • Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents
  • Synthetic Methods, Chemistry, and the Anticonvulsant Activity of Thiadiazoles

Table 3 shows the hydrogen bonding distances of the reported thiadiazole series of compounds. The residues obtained from these studies were compared with the previous reported docking study of thiadiazole compounds [ 910 ].

thiadiazole synthesis

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The compounds thiadiazole synthesis ranked as per the docking score. This docking study reveals the importance of amino acid residues found to have significant interactions.


From this study it was observed that compounds that have lowest thiadiazole synthesis bonding distances with Ser are also higher active amongst the selected series of thiadiazole compounds Figure 3. Distances larger than 3.

Synthesis of 1,3,4-thiadiazoles

The lower activity of these compounds may be due to weaker binding interactions. Table 4 consists of first seven virtually designed molecules that were selected based on no steric clash and lower GScore values.

Thiadiazole synthesis was found to have hydrogen boning with Cys thiadiazole synthesis which sulfer H-bonds with nitrogen of thiadiazole ring system.


TD4 shifts away from Ser and forms H-bond with Arg The bending is thiadiazole synthesis to absence of double bond linkage in the molecule TD7.

Such interaction is not possible in TD1 to TD6. Thiadiazole synthesis rich substitutions on Ar position shifts the molecule towards other side of the cavity i.

TD4 has no H-bonding with Ser and drifts towards Arg Thiadiazole synthesis group substitutions that vary from acetyl or methyl group of toluidine showed no steric clashes with Ile Spectral Data of synthesized compounds Table 6 gives the characterization data of thiadiazole synthesis synthesized compounds.

N- 5- 4-nitrophenyl -1,3,4-thiadiazolyl acetamide: N- 4-nitrobenzilidene phenyl-1,3,4- thiadiazolamine: CH10 S, -CH. N- 4-chlorobenzylidene 4-aminophenyl - 1,3,4thiadiazolamine: N- 4-chlorobenzylidene phenyl-1,3,4- thiadiazolamine: N- 4-fluorobenzylidene 4-aminophenyl - 1,3,4-thiadiazolamine: In vitro activity In vitro studies carried out on porcine alpha amylase showed that out of all molecules TD1 was found most potent.

thiadiazole synthesis


Acarbose, alphaglucosidase inhibitor was used as standard in vitro study. Acarbose lowers the rate of glucose absorption through delayed carbohydrate digestion thiadiazole synthesis extended digestion time.

Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents | OMICS International

Scheme 18 2 Nucleophilic Thiadiazole synthesis. Due to the electronegativity of the two nitrogen thiadiazole synthesis in the ring, the carbon atom has low electron density and gives many possible nucleophilic reactions [ 18 ].

Halogenate 1,3,4-thiadiazoles are important intermediates in which the halogen atom is readily by nucleophiles.

Scheme 19 Amino thiadiazoles are rather weak bases; they are nucleophilic enough to be readily acetylated by acid chlorides or acetic acids Scheme