High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

The 1,3,4-thiadiazole nucleus is one of the most important and well-known heterocyclic nuclei, which is a common and integral feature of a variety of natural products and medicinal agents. Thiadiazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, and antitubercular agents. The broad and potent activity of thiadiazole and their derivatives has established them as pharmacologically significant scaffolds. In this study, an attempt has been made with recent research findings on this nucleus, to review the structural modifications on different thiadiazole derivatives for various pharmacological activities.

https://onlinelibrary.wiley.com/doi/pdf/10.1111/cbdd.12125

1,3,4-thiadiazole and its derivatives: a review on recent progress in biological activities.

Metal complexes of Schiff base: Preparation, characterization and antibacterial activity

Pathogenic microorganisms are causative agents for different types of serious and even lethal infectious diseases. Despite advancements in medication, bacterial and fungal infections continue to be a growing problem in health care. As more and more bacteria become resistant to antibiotics used in therapy and an increasing number of invasive fungal species become resistant to current antifungal medications, there is considerable interest in the development of new compounds with antimicrobial activity. The compounds containing a heterocyclic ring play an important role among organic compounds with biological activity used as drugs in human and veterinary medicine or as insecticides and pesticides in agriculture. Thiadiazoles belong to the classes of nitrogen-sulfur heterocycles with extensive application as structural units of biologically active molecules and as useful intermediates in medicinal chemistry. The potency of the thiadiazole nucleus is demonstrated by the drugs currently used. 1,3,4-Thiadiazoles and some of their derivatives are extensively studied because of their broad spectrum of pharmacological activities. The aim of this review was to highlight the main antimicrobial properties exhibited by derivatives possessing 2-amino-1,3,4-thiadiazole moiety. Many of the reported 2-amino-1,3,4-thiadiazole derivatives can be considered as lead compounds for drug synthesis, and several of them have demonstrated higher antimicrobial activity in comparison to standard drugs. Furthermore, taking into account the reactivity of the amine group in the derivatization process, 2-amino-1,3,4-thiadiazole moiety may be a good scaffold for future pharmacologically active 1,3,4-thiadiazole derivatives.

/pdf/2-amino-1-3-4-thiadiazole-as-a-potential-scaffold-for-7g57aig1u9.pdf

2-Amino-1,3,4-thiadiazole as a potential scaffold for promising antimicrobial agents.

High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv.

Synthesis of α-[5-(5-amino-1,3,4-thiadiazol-2-yl)-2-imidazolylthio]acetic acids

The paper describes synthesis and antituberculosis activity of α-[5-(5-amino-1,3,4-thiadiazol-2-yl)-imidazol-2-ylthio]acetic acids (5a,b). The compounds were tested against Mycobacterium tuberculosis strain H37Rv in comparison to rifampicin. Compounds exhibited low activity (MIC ≤ 6.25 μg/ml, % inhibition ≥ 24).

Rahil Vosooghi

Papers

Synthesis of α-[5-(5-amino-1,3,4-thiadiazol-2-yl)-2-imidazolylthio]acetic acids

Synthesis of α-[5-(5-Amino-1,3,4-thiadiazol-2-yl)-2-imidazolylthio]acetic Acids.