Substituted benzyl-pyrimidines targeting thymidine monophosphate kinase of Mycobacterium tuberculosis: Synthesis and in vitro anti-mycobacterial activity

Antitubercular drugs: advances in nitrogen containing heterocyclic compounds and some other derivatives

“…TMPK inhibitors have (21) on TMPKmt showed that the hydrogen of the thymine and acid group can interact with Arg95. 30 Pyridine derivatives have also been illustrated as anti--TB agents, compound (22), presenting inhibitory activity with an IC50 value of 0.38 μM, being its possible mechanism of action through glutamine synthetase inhibition. This would be the first inhibitor compound not derived from amino acids against the proposed target.…”

“…The modifications of benzofuro benzopyran have showed less active compounds such as compound (30), where the furan B ring is replaced by an ether linker, a carbonyl group, a hydroxy methylene or a methylene group. The modifications such as acylation and bromination in 5--position on the C ring have produced inactive compounds.…”

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

“…In particular benzyl-thymine derivatives have been remarkable TMPK inhibitors, which has led to the proposal of new modifications such as: chain length in para-position on the benzyl ring, saturation of the alkyl chain, functionalization of the chain group and substitution at 5- figure 16) on TMPKmt showed that the hydrogen of the thymine and acid group can interact with Arg95 (Gasse et al, 2008). Pyridine derivatives have also been described as anti-TB agents, an example is compound 53 (figure 17), which presents inhibitory activity with an IC50 value of 0.38 µM, suggesting that its possible mechanism of action is through glutamine synthetase inhibition.…”

Synthesis and Spectral Analysis of an Array of Novel 4-(4-Morpholinophenyl)-6-Aryl-Pyrimidin-2-Amines

“…Some notable biological activity of pyrimidine derivatives include adenosine receptor antagonists [1], kinase inhibitors [2], analgesic [3], anti-inflammatory [3], inhibitors of cyclin-Dependent kinases 1 and 2 [4], calcium channel antagonist [5], antihistaminic [6], antitubercular [7] activities. Substituted aminopyrimidine nuclei are common in marketed drugs such as anti-atherosclerotic aronixil, anti-histaminic thonzylamine, anti-anxielytic buspirone, anti-psoriatic enazadrem, and other medicinally relevant compounds.…”