19819-17-1Relevant articles and documents
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis
Samala, Ganesh,Brindha Devi, Parthiban,Saxena, Shalini,Gunda, Saritha,Yogeeswari, Perumal,Sriram, Dharmarajan
, p. 5556 - 5564 (2016/10/24)
Thirty three derivatives of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues were synthesized by molecular modification of a reported antimycobacterial molecule (GSK163574A). Compounds were evaluated in vitro against actively replicative and nutrient starved non-replicative Mycobacterium tuberculosis (MTB), enzymatic screening and cytotoxicity against RAW 264.7 cell line. Among the compounds, 2-ethyl-N-phenethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine (5c) was found to be the most active compound against non-replicative MTB with 2.7 log reduction of bacteria at 10?μg/mL and was more potent than isoniazid (1.2 log reduction) and rifampicin (2.0 log reduction) at same dose level. Compound 5c also showed activity against MTB alanine dehydrogenase enzyme with IC50of 1.82?±?0.42?μM and showed 25% cytotoxicity against RAW 264.7 cell line at 50?μg/mL.
Utility of a 2-Aminothiophene-3-carboxamide in the synthesis of thienopyridines and thienopyrimidines
Mohareb, Rafat M.,Sherif, Sherif M.,Gaber, Hatem M.,Ghabrial, Sami S.,Aziz, Susan I.
, p. 459 - 467 (2007/10/03)
The article discussed about the utility of a 2-aminothiophene-3-carboxamide in the synthesis of Theinopyridines and theinopyrimidines. The reactivity of the compound toward a variety of chemical reagents was studied. The reaction mixture was evaporated in vacuo and triturated with cold water, whereby the resulting solid product was collected by filtration and crystallized from the proper solvent.