AI Article Synopsis

  • A new series of compounds called 4,7-dihydro-[1,2,3]thiadiazolo[5,4-b]pyridine-6-carboxamides were created using a simple one-pot reaction involving specific chemicals and no catalysts, leading to moderate to good yields.
  • The synthesized compounds were tested for antimicrobial activity, with 4e showing greater effectiveness against a harmful type of bacteria than ciprofloxacin, and 4d proving more potent against Candida albicans than Amphotericin B.
  • Further analysis revealed that compound 4e had a strong binding affinity to its receptor, highlighting its potential as a safe and effective treatment for fungal and bacterial infections.

Article Abstract

A diverse set of 4,7-dihydro-[1,2,3]thiadiazolo[5,4-b]pyridine-6-carboxamides 4(a-o) was synthesized via a one-pot reaction of 5-amino-[1,2,3]thiadiazole, various aromatic aldehydes, and different acetoacetanilides, using glacial acetic acid. The resulting compounds were obtained in moderate to good yields. All the newly synthesized compounds were evaluated for their antimicrobial activity. Among them, compound 4 e demonstrated superior efficacy against the Salinivibrio proteolyticus strain of Gram-negative bacteria compared to ciprofloxacin. Compound 4 d exhibited the highest potency against the fungal strain Candida albicans, surpassing amphotericin B. The physicochemical characteristics of 4 d and 4 e were assessed. According to docking analysis, DHTDAPy 4 e shows a higher binding affinity of -7.2 kcal/mol in the binding cavity of the receptor. These findings illustrate the safety, tolerability, and potency of the newly synthesized DHTDAPy compounds against fungal and bacterial infections.

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http://dx.doi.org/10.1002/cmdc.202400595DOI Listing

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