A Sorbitol Dehydrogenase Inhibitor of Exceptional in Vivo Potency with a Long Duration of Action:  1-(R)-{4-[4-(4,6-Dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl}ethanol

Abstract

We report here a novel sorbitol dehydrogenase inhibitor, 16, that shows very high oral potency (50 microg/kg) in normalizing elevated fructose levels in the sciatic nerve of chronically diabetic rats and sustained duration of action (>24 h). Furthermore, 16 shows attractive pharmaceutical properties, including good solubility in simulated human gastric fluid, excellent Caco-2 Papp, moderate lipophilicity, and metabolic stability for achieving good oral absorption and long duration of action.

Water-soluble DNA minor groove binders as potential chemotherapeutic agents: synthesis, characterization, DNA binding and cleavage, antioxidation, cytotoxicity and HSA interactions

“…in the body. Therefore, triazines and their derivatives have a wide range of biological activities, such as antibacterial, 11 antitrypanosome, 12 antitumor, 13 antiretrovirus, 14 antagonism, 15 inhibition of sorbitol dehydrogenase, 16 and adjusting the estrogen receptor. 17 In recent years, diamino-s-triazine (DAT) derivatives have attracted much attention for their prominent anti-angiogenesis and antitumor activities.…”

A Trinuclear Copper(II) Complex of 2,4,6-Tris(di-2-pyridylamine)-1,3,5-triazine Shows Prominent DNA Cleavage Activity

“…Derivatives of 1,3,5-triazine have exhibited promising potential as antitumor agents, enzyme inhibitors, and other bioactive agents . However, their metal complexes received little attention for biological applications partly due to their poor solubility in both water and common organic solvents …”

Synthesis, characterization and in vitro biological evaluation of some new 1,3,5-triazine-bis-azomethine hybrid molecules as potential antitubercular agents

“…Recently, 2,4,6-trisubstituted-1,3,5-triazine scaffolds were discovered as a potent inhibitors of Mycobacterium tuberculosis H37Rv [10]. Currently 1,3,5-triazine derivatives have been found to possess wide range of biological activities, such as adenosine receptor antagonist [11], antiamoebic [12], anticancer [13], antileishmanial [14], antimalarial [15], antimicrobial [16], antiviral [17], antitubercular [18], carbonic anhydrase inhibitor [19], cathepsin B inhibitor [20], cholesteryl ester transfer protein inhibitor [21], corticotropin-releasing factor ligand [22], CRF1 PET imaging agent [23], cytosolic phospholipase A2α inhibitor [24], dipeptidyl peptidase IV inhibitor [25], bacterial enzyme DNA helicase inhibitor [26], dual PI3/mTOR inhibitor [27], glucocerebrosidase inhibitor [28], α-glucosidase inhibitor [29], growth factor inhibitor [30], human gonadotropin-releasing hormone receptor antagonist [31], 5-HT7 receptor antagonist [32], inosine monophosphate dehydrogenase inhibitor [33], mTOR kinase inhibitor [34], voltage-gated sodium channel Nav 1.7 antagonist [35], neuronal voltage-gated sodium channel blocker [36], phosphodiesterase type 4 inhibitor [37], protein kinase CK2 inhibitor [38], ROCK inhibitor [39], β-secretase inhibitor [40], sorbitol dehydrogenase inhibitor [41], tryptophan hydroxylase inhibitor [42] and VLA-4 integrin antagonist [43]. Similarly, azomethine moiety has gained a great importance, since it has been found to possess several biological activities, such as antimicrobial [44]…”