AbstractOver the past few decades, the dynamic progress in the synthesis and screening of heterocyclic compounds against various targets has made a significant contribution in the field of medicinal chemistry. Among the wide array of heterocyclic compounds, triazole moiety has attracted the attention of researchers owing to its vast therapeutic potential and easy preparation via copper and ruthenium‐catalyzed azide‐alkyne cycloaddition reactions. Triazole skeletons are found as major structural components in a different class of drugs possessing diverse pharmacological profiles including anti‐cancer, anti‐bacterial, anti‐fungal, anti‐viral, anti‐oxidant, anti‐inflammatory, anti‐diabetic, anti‐tubercular, and anti‐depressant among various others. Furthermore, in the past few years, a significantly large number of triazole hybrids were synthesized with various heterocyclic moieties in order to gain the added advantage of the improved pharmacological profile, overcoming the multiple drug resistance and reduced toxicity from molecular hybridization. Among these synthesized triazole hybrids, many compounds are available commercially and used for treating different infections/disorders like tazobactam and cefatrizine as potent anti‐bacterial agents while isavuconazole and ravuconazole as anti‐fungal activities to name a few. In this review, we will summarize the biological activities of various 1,2,3‐triazole hybrids with copious oxygen‐containing heterocycles as lead compounds in medicinal chemistry. This review will be very helpful for researchers working in the field of molecular modeling, drug design and development, and medicinal chemistry.

01 Dec 2022·European Journal of Medicinal Chemistry

1,2,3-Triazole-containing hybrids with potential antibacterial activity against ESKAPE pathogens

Review

Author: Wang, Jun ; Yan, Heng ; Liu, Bao-Shan ; Liu, Kai ; Shi, Yu-Min ; Deng, Cui

ESKAPE pathogens, as priority 1 and 2 pathogens, are prevalent infectious agents associated with high morbidity and mortality. ESKAPE can cause broad-spectrum diseases with increasing tendency of resistance acquisition to antibiotics and have enhanced the urge for the development of alternate therapeutics. 1,2,3-Triazole, a highly privileged moiety for the discovery of novel drugs, not only can act as a linker to tether different pharmacophores, but also can serve as a pharmacophore. Notably, several 1,2,3-triazole-containing hybrids which are exemplified by cefatrizine, radezolid and tazobactam have already approved as antibiotics to treat infections caused by various organisms including ESKAPE pathogens and their drug-resistant forms, revealing that 1,2,3-triazole-containing hybrids are useful prototypes for clinical deployment in the control of bacterial infections. The purpose of the present review article is to provide an emphasis on the current scenario (2018-2022) of 1,2,3-triazole-containing hybrids with potential antibacterial activity against ESKAPE pathogens to facilitate further rational design of more effective candidates.

01 Jan 2022·Current Topics in Medicinal ChemistryQ4 · MEDICINE

The Antibacterial Activity of 1,2,3-triazole- and 1,2,4-Triazole-containing Hybrids against Staphylococcus aureus: An Updated Review (2020- Present)

Q4 · MEDICINE

Review

Author: Zhang, Junwei ; Li, Jie

Abstract:Staphylococcus aureus (S. aureus), a prominent, highly contagious nosocomial and com-munity-acquired bacterial pathogen, can cause a broad spectrum of diseases. Antibiotic-resistant S. aureus strains, which pose potential causes of morbidity and mortality, have continuously emerged in recent years, calling for novel anti-S. aureus agents. 1,2,3-Triazole and 1,2,4-triazole, the bioisostere of amides, esters, and carboxylic acids, are potent inhibitors of DNA gyrase, topoisomerase IV, efflux pumps, filamentous temperature-sensitive protein Z, and penicillin-binding protein. In particular, 1,2,3-triazole- and 1,2,4-triazole-containing hybrids have the potential to exert dual or multiple anti-bacterial mechanisms of action. Moreover, 1,2,3-triazole-cephalosporin hybrid cefatrizine, 1,2,3-triazole-oxazolidinone hybrid radezolid, and 1,2,4-triazolo[1,5-a]pyrimidine hybrid essramycin, have already been used in clinical practice to treat bacterial infections. Hence, 1,2,3-triazole- and 1,2,4-triazole-containing hybrids possess promising broad-spectrum antibacterial activity against diverse clinically significant organisms, including drug-resistant forms. This review is an update on the latest development of 1,2,3-triazole- and 1,2,4-triazole-containing hybrids with anti-S. aureus activity, cov-ering articles published between January 2020 and July 2021.

100 Deals associated with Cefatrizine

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KEGG	Wiki	ATC	Drug Bank
D02406	Cefatrizine	J01DB07	DB13266

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Indication	Country/Location	Organization	Date
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