Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480
Pursuing our search program for new antitubercular drugs we decided to explore the potentiality of oxazolidinone moiety by synthesizing novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480. The new derivatives were tested against atypical mycobacteria as well as against drug resistant Mycobacterium tuberculosis and some of them exhibited a fairly good activity against Mycobacterium avium complex (MAC).
Sbardella, Gianluca,Mai, Antonello,Artico, Marino,Loddo, Roberta,Setzu, Maria Grazia,La Colla, Paolo
p. 1537 - 1541
(2007/10/03)
Novel HIV-1 protease inhibitors active against multiple PI-Resistant viral strains: Coadministration with indinavir
HIV-1 protease inhibitors (PI) with an N-arylpyrrole moiety in the P 3 position afforded excellent antiviral potency and substantially improved aqueous solubility over previously reported variants. The rapid in vitro clearance of these compounds in human liver microsomes prompted oral coadministration with indinavir to hinder their metabolism by the cyctochrome P450 3A4 isozyme and allow for in vivo PK assessment.
Kevin, Nancy J.,Duffy, Joseph L.,Kirk, Brian A.,Chapman, Kevin T.,Schleif, William A.,Olsen, David B.,Stahlhut, Mark,Rutkowski, Carrie A.,Kuo, Lawrence C.,Jin, Lixia,Lin, Jiunn H.,Emini, Emilio A.,Tata, James R.
p. 4027 - 4030
(2007/10/03)
Polycondensed heterocycles. VII. A convenient synthesis of pyrrolo[1,2-a]quinoxaline derivatives by intramolecular aromatic nucleophilic displacement
4-(4-Methyl-1-piperazinyl)-7- trifluoromethylpyrrolo[1,2-a]quinoxaline (CGS 12066B) and related analogs were prepared in good overall yield through a reaction sequence involving as a key step in the intramolecular substitution of aromatic fluoride or nitr
Campiani,Nacci,Corelli,Anzini
p. 1567 - 1576
(2007/10/02)
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