Synthesis of Benzazolyl Pyrimidines Under Ultrasonication and Their Antimicrobial Activity

Kayathi, Narendra Babu; Sowmya, Donthamsetty V.; Padmaja, A.; Padmavathi, V.

doi:10.1002/jhet.3134

Cited by 6 publications

(2 citation statements)

References 26 publications

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“…Next, novel benzoxazolyl, benzothiazolyl and benzimidazolyl pyrimidines derivatives were synthesized and evaluated by Kayathi et al [21] Among them, compounds 23 and 24 (Figure 4) with benzothiazolyl and benzimidazolyl groups, respectively, both exhibited the equivalent potent activity against B. subtilis and A. niger compared to that of standard drug chloramphenicol and ketoconazole. The electron-withdrawing groups such as nitro group on the benzene ring was found to increase the activity.…”

Section: Monopyrimidine Trisubstituted Derivativesmentioning

confidence: 99%

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Zhuang

2020

ChemMedChem

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Multidrug-resistant bacterial infections have become an important cause of clinical death in the twenty-first century. Much effort has been made to overcome this challenge. The discovery of novel antimicrobial compounds, as well as the rational use of antibacterial drugs with different structure types and mechanisms, is helping to deal with bacterial resistance. Currently, pyrimidine-containing agents are the major areas of new antibacterial drug discovery. Given their good activities and diverse mechanisms of action, many pyrimidine-containing heterocyclic compounds have become the focus of interest for many scientists. In addition, pyrimidine structure is an important part of many endogenous substances, which is an advantage that allows pyrimidine derivatives to interact with genetic materials, enzymes and other biopolymeric substances in the cell. Scientists have focused on the discovery and structural optimization of pyrimidine derivatives, which has resulted in the discovery of many novel pyrimidine derivatives with intriguing profiles. Herein we summarize the therapeutic potentials of pyrimidine compounds that are promising for antimicrobial applications over the last decade. In particular, the relationships between the structures of modified pyrimidines and their antimicrobial activity are systematically discussed.

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Section: Monopyrimidine Trisubstituted Derivativesmentioning

confidence: 99%

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Zhuang

2020

ChemMedChem

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“…It has been reported that pyrimidine and its fused pyrimidine derivatives are a class of heterocyclic scaffolds that possess a range of biological and pharmacological activities, 1 for example, anticancer, 2 antimicrobial, 3 antioxidant, 4 antidepressant, 5 antiviral, 6 and anxiolytic activities. 7 Because of the extensive pharmacological and biological activities of pyrimidine, 8 the action targets of pyrimidine were conducted in-depth studies.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Biological Evaluation of Pyrimidinamine Derivatives Containing Urea Moiety

Wang¹,

Ouyang²,

Liu³

et al. 2023

HETEROCYCLES

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New series of 17 pyrimidinamine derivatives containing urea moiety were designed and synthesized. Their antitumor activity was investigated by MTT method. The results showed that some of these compounds exhibited moderate to good antitumor activities against all four cancer cell lines. The IC50 value of compound HD-6 on PC-3 cells was better 2.37 μM than the positive control drug sorafenib (3.66 μM). The inhibitory activity of most target compounds on HepG2 cells was better than that of positive drug sorafenib (10.70 μM). Among them, the IC50 value of compound HD-6 on K562 cells was 6.80 μM, which close to solafinib (4.62 μM). Further studies revealed that compound HD-6 clearly possessed apoptosis inducing effects, increased the level of reactive oxygen species, arrested the cycle in the G2/M phase and regulated the expression of tyrosine kinase EGFR in PC-3 cells.

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