1,2,4-Triazine nucleus is a prominent structural core system present in numerous pharmacologically active compounds. Till date, various 1,2,4-triazine analogs, possesing a wide range of potent pharmacological activities, have been reported. This review is an attempt to compile the medicinal chemistry aspects of various synthesized 1,2,4-triazine analogs reported so far.
1,2,3-Triazine is an interesting class of heterocyclic compounds. Various synthetic analogs of 1,2,3-triazine have been prepared and evaluated for many pharmacological activities in different models with desired findings. Some analogs have shown potent pharmacological activity and may be considered as lead molecule for the development of future drugs. This review is an attempt to organize the chemical and pharmacological aspects of 1,2,3-triazine analogs reported till date systematically since 1970.
A series of substituted 1-hydroxy-2-naphthanilides 4--14 has been synthesized by treating 1-hydroxy-2-naphthoic acids 2 with substituted anilines 3. The nitronaphthanilides, on reduction and subsequent treatment with thiophosgene, gave the corresponding substituted 2-naphthanilide isothiocyanates 30--33. Substitution of the chlorine of 8 by various cyclic amines gave 3'-nitro-4'-substituted 1-hydroxy-2-naphthanilides 15--21. Various 3-aryl-4-oxo-2,3-dihydro-1,3-naphthoxazine-2-thiones 34-43 and 3 aryl-2,4-dioxo-2,3-dihydro-1,3-naphthoxazines 44--51 have been prepared by reacting the corresonding naphthanilides with thiophosgene and ethyl chloroformate, respectively. All the compounds were tested for their cestodicidal activity against Hymenolepis nana infection in rats; 30 was found to be the most active compound of the series, showing 100% clearance of infection at a single oral dose of 7.5 mg/kg.
Aim: To design, synthesize and evaluate the hypoglycemic activity of a new class of 7-hydroxy Coumarin derivatives. Background: Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effective and efficient therapeutic anti-diabetic agents is continuing. Recent studies support the search for coumarins or related compounds with potential blood glucose-lowering properties. Objective: To explore and establish the in-silico-driven pharmacological role of a new class of 7-hydroxy Coumarin derivatives as the therapeutic strategies against type 2 diabetes mellitus. Material and methods: A new class of 7-hydroxy Coumarin derivatives was designed by assessment of their physicochemical properties and molecular docking against the Glucagon-like peptide-1 (GLP-1) receptor. Two novel series of 30 compounds were synthesized. The chemical structures of all the synthesized analogues have been elucidated by spectral studies of IR, 1H-NMR, and mass spectroscopy. After considering the molecular docking score and their physicochemical properties, the compounds were screened out for the evaluation of their hypoglycemic potential. The compounds were investigated for their hypoglycemic activity using a streptozotocin (STZ) induced diabetic model and an oral glucose tolerance test (OGTT) method at different dose levels. Result: The molecular docking studies of synthesized derivatives reveal significant molecular interaction with the various amino acid residues of GLP-1 receptor. IR spectral analysis revealed a strong band of -NH stretching in the range of 3406.7-3201.61 cm-1 and one strong band for the lactone carbonyl group of the coumarin ring in the range of 1722.0-1703.5 cm-1, confirming the chemical structure of all produced compounds. The synthesized coumarin analogues with the best docking score exhibited remarkable hypoglycemic potential as assessed by STZ model and the OGTT method. Conclusion: good structure-activity relationship (SAR) and produced significant hypoglycemic potential.
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