743420-78-2Relevant academic research and scientific papers
GUANIDINE COMPOUNDS AND USE THEREOF
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Page/Page column 25; 38, (2015/11/09)
The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.
Synthesis and antimicrobial activity of N1-benzyl or N 1-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines
Ma, Xiang,Tan, Soo-Tong,Khoo, Chai-Ling,Sim, Hong-May,Chan, Lai-Wah,Chui, Wai-Keung
, p. 5428 - 5431 (2011/10/12)
The emergence and spread of multidrug-resistant strains of Staphylococcus aureus and Mycobacterium tuberculosis are generating a threat to public health worldwide. In the current study, a series of N1-benzyl and N 1-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamine derivatives were synthesized and investigated for their antimicrobial activity against S. aureus, and Mycobacterium smegmatis which is taxonomically related to M. tuberculosis. Most of the compounds exhibited good activity against M. smegmatis as determined by comparison of diameters of the zone of inhibition of test compounds and standard antibiotics. Compound 7o showed potent antimycobacterial activity against M. smegmatis without mammalian DHFR inhibition liability. The results from this study indicate that 1-benzyl derivatives of 1,6-dihydro-1,3,5- triazine-2,4-diamines may be used as lead compounds for the discovery of antimycobacterial agents.
Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers
Ma, Xiang,Poon, Thong-Yuen,Wong, Peter Tsun Hon,Chui, Wai-Keung
supporting information; experimental part, p. 5644 - 5647 (2010/04/26)
Neuronal sodium channels blockers interfere with ion flux and have been used for managing neuropathic pain, epilepsy, and cerebral ischemic disorders. In the current study, four groups of 2,4-diamino-1,3,5-triazine derivatives were synthesized and investigated for their neuronal sodium channels binding activity. 5-Aryl-1,3,5-triazaspiro[5.5]undeca-1,3-diene-2,4-diamines (4a-4j) were found to have the best neuronal sodium binding activity among the four groups of triazines evaluated. Derivatives 4a-4j blocked the sodium channels with IC50 values ranged from 4.0 to 14.7 μM. The result from this study showed that analogues of 2,4-diamino-1,3,5-triazines could be used as leads for the discovery of neuronal sodium channels blockers for managing central nervous system related disorders.
