The reaction of 5-amino-3-(arylamino)-1H-pyrazole-4-carboxamides 1a,b with acetylacetone 2 and arylidenemalononitriles 5a-c yielded the pyrazolo[1,5-a]-pyrimidine derivatives 4a,b and 7a-f respectively. On the other hand, Schiff bases 9a,b and 12a-j were obtained upon treatment of carboxamides 1a,b with isatin 8 and some selected aldehydes 11a-e. The newly synthesized compounds were characteriz...

Optically active isomers of N-methy1-2-(2-(2-(4-phenylpiperazino)ethoxy)phenyl)thiazolidine3-carboxamides(( + )-2 and(-)-2) have been synthesized and tested for positive inotropic activity. The racemic thiocarboxamide((•})-3) was resolved into the enantiomers(( + )-3 and(•E)-3) via the Land D-N-(2-naphthylsulfonyl)prolyl derivatives ((+ )-4 and (-)-4). Conversion of the thiocarboxamides (( + )-...

We describe an isomerization-alternating ROMP protocol that gives linear copolymers with rigorous sequence alternation. Bicyclo[4.2.0]oct-7-ene-7-carboxamides of primary amines are isomerized in the presence of (3-BrPyr)2Cl2(H2IMes)Ru=CHPh to the corresponding bicyclo[4.2.0]oct-1(8)-ene-8-carboxamides in which the olefinic bond is tetrasubstituted. The isomerized amides undergo alternating ring...

A series of N-alkyl-3-(alkylamino)pyrazine-2-carboxamides and their N-alkyl-3-chloropyrazine-2-carboxamide precursors were prepared. All compounds were characterized by analytical methods and tested for antimicrobial and antiviral activity. The antimycobacterial MIC values against Mycobacterium tuberculosis H37Rv of the most effective compounds, 3-(hexylamino)-, 3-(heptylamino)- and 3-(octylami...

2-Oxo-4-phenyl-1,2,5,6,7,8-hexahydroquinoline-3-carbonitrile (10) reacted with hydrazine hydrate, phenylisothiocyanate or benzoyl chloride to give derivatives 12, 13 and 15, respectively. The latter two products were treated with hydrazine hydrate to afford pyrozole[3,4-b]quinolines derivatives 14 and 16, respectively. Compound 10 also reacted with acetonitrile dimer or malononitrile dimer to y...

Halonium-initiated cascade reaction of 1-alkenoylcyclopropane carboxamides was developed, which leads to the production of dihydrofuropyridinones and 3(2H)-furanones, respectively, depending on the property of substituents on the enone moiety.

Integrase (IN) inhibitors are the newest class of antiretroviral agents developed for the treatment of HIV-1 infections. Merck's Raltegravir (RAL) (October 2007) and Gilead's Elvitegravir (EVG) (August 2012), which act as IN strand transfer inhibitors (INSTIs), were the first anti-IN drugs to be approved by the FDA. However, the virus develops resistance to both RAL and EVG, and there is extens...