Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

The antibacterial activities of a series of triazolyl oxazolidinones against Mycobacterium tuberculosis strain in vitro and in vivo in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC90: < 0.2 to 0.422 μg/mL) and arylcarbonyl (IC90: < 0.2 to 2.103 μg/mL) groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC90: < 0.2 μg/mL) analog, linezolid (IC90: < 0.2 μg/mL), and isoniazid (IC90: < 0.034 μg/mL). The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27) derivative with medium bioavailability in plasma was most active in vivo, but relatively less efficacious than isoniazid

Effect of Nano-Silica on the Physical, Mechanical and Thermal Properties of the Natural Rubber Latex Modified Concrete

The preparation and properties of latex modified concrete (LMC), nano silica modified concrete (nSMC) and silica-latex modified concrete (SLMC) have been investigated in this study. Properties like compressive strength, tensile strength, flexural strength, thermal characteristics and water absorption have been evaluated. The 7-day compressive strength has increased 37% (30.15 N/mm2) after the inclusion of nano silica and latex. The composite has showed considerable improvements in splitting tensile strength (3.24 N/mm2), flexural strength (6.05 N/mm2) and thermal conductivity, while it lowered the water absorption rate. The property increase has been attributed to the pore filling and pozzolanic activity of nano silica and densification of matrix by natural rubber latex and nano silica. The results of this study have suggested that the addition of nano silica and latex could be a relevant technique toward conventional concrete as a key material along with energy efficient construction and building technology

Effect of Nano-Silica on the Physical, Mechanical and Thermal Properties of the Natural Rubber Latex Modified Concrete

452-457The preparation and properties of latex modified concrete (LMC), nano silica modified concrete (nSMC) and silica-latex modified concrete (SLMC) have been investigated in this study. Properties like compressive strength, tensile strength, flexural strength, thermal characteristics and water absorption have been evaluated. The 7-day compressive strength has increased 37% (30.15 N/mm2) after the inclusion of nano silica and latex. The composite has showed considerable improvements in splitting tensile strength (3.24 N/mm2), flexural strength (6.05 N/mm2) and thermal conductivity, while it lowered the water absorption rate. The property increase has been attributed to the pore filling and pozzolanic activity of nano silica and densification of matrix by natural rubber latex and nano silica. The results of this study have suggested that the addition of nano silica and latex could be a relevant technique toward conventional concrete as a key material along with energy efficient construction and building technology

Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

The antibacterial activities of a series of triazolyl oxazolidinones against Mycobacterium tuberculosis strain in vitro and in vivo in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC 90 : &lt; 0.2 to 0.422 μg/mL) and arylcarbonyl (IC 90 : &lt; 0.2 to 2.103 μg/mL) groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC 90 : &lt; 0.2 μg/mL) analog, linezolid (IC 90 : &lt; 0.2 μg/mL), and isoniazid (IC 90 : &lt; 0.034 μg/mL). The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27) derivative with medium bioavailability in plasma was most active in vivo, but relatively less efficacious than isoniazid