Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2′-‘up’ fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors

Novel 5′-Norcarbocyclic Pyrimidine Derivatives as Antibacterial Agents

“…In contrast, the observed biological activity of these new derivatives of 5-substituted uracils are in good correlation with previously reported data on the inhibition of M.tb growth by nucleoside analogues containing 5-substituted pyrimidine bases and different sugars, as well as their corresponding acyclic, or carbocyclic analogues [4,5,15,16,17,18,53] As a result, it appears these compounds may have the same mechanism of antimicrobial action (likely cell wall disruption) and that it depends primarily on the length and structure of the substituent at C-5 of the base moiety. Thus this new data has added to the growing examples of similar compounds and their mechanism of action for inhibitors of this type.…”

“…Nucleoside derivatives have historically served as potent antiviral and anticancer agents [3], but it was not until 2000 that their anti-TB activity was reported [4]. Recently, several reports of modified nucleosides showing activity against Mycobacterium tuberculosis (M. tuberculosis) , Mycobacterium bovis (M. bovis) and Mycobacterium avium (M. avium) were published [4,5,6,7,8,9,10,11,12,13,14,15,16,17,18]. Among them, the best activity was observed for several uridine analogues (MIC 90 1 to 10 µg/mL) possessing 5-alkynyl (decynyl, dodecynyl, tetradecynyl, pyridylethynyl, etc.)…”

Exploration of the Chemistry and Biological Properties of Pyrimidine as a Privilege Pharmacophore in Therapeutics

“…Imidazo[1,2-c]pyrimidin-4-ol emerged as the most potent among the series screened by Barot et al (2014) against M. tuberculosis H 37 Rv. According to Shakya et al (2012), Fig. 39: Selected pyrimidine moieties with antiviral activity Int.…”

Spectral Characterization and Vibrational Assignments of Ethyl 4-(3-(2,3-Dihydrobenzofuran-5-Carboxamido)Phenyl) -6-Methyl-2-Oxo-1,2,3,4-Tetrahydropyrimidine-5- Carboxylate by Ab Initio Density Functional Method

“…It have wide range of biological activities 1,2 . Such as, anti-leishmanial 3 , anti-tuberculosis 4 , analgesic, anti-inflammatory [5][6][7] , antimicrobial 8 , antifungal 9 anti-emetic 10 and antitumor properties 11 . The nonlinear optical active molecules with p _ conjugated backbones, electron donating, electron withdrawing moieties are important class of materials in modern technologies, such as telecommunication and optoelectronics 12 ,multiphoton microscopy 13 , Organic light-emitting diodes (OLED) 14 , organic field effect transistors (OFET) 15 and to achieve hierarchical self-assembly in "all-organic" photovoltaic devices 16 Here, we report synthesis of a new nonlinear molecule ethyl ethyl 4-(3-(2,3-dihydrobenzofuran-5-carboxamido)phenyl)-1,2,3,4-tetrahydro-6-methyl-2-oxopyrimidine-5-carboxylate(DFOC).…”