40310-35-8Relevant articles and documents
Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis
Singh, Priyanka,Manna, Sudipta Kumar,Jana, Amit Kumar,Saha, Tiash,Mishra, Pankaj,Bera, Saurav,Parai, Maloy Kumar,Srinivas Lavanya Kumar,Mondal, Sankalan,Trivedi, Priyanka,Chaturvedi, Vinita,Singh, Shyam,Sinha, Sudhir,Panda, Gautam
, p. 357 - 368 (2015/04/14)
Triarylmethanes (TRAMs) and thiophene containing trisubstituted methanes (TRSMs) have been reported by us, having potential against Mycobacterium tuberculosis and Mycobacterium fortuitum strains, respectively. Further, extension through synthesis and biol
Design, synthesis and antitubercular activity of compounds containing Aryl and heteroaryl groups with alkylaminoethyl chains
Panda, Gautam,Parai, Maloy Kumar,Srivastava, Ajay Kumar,Chaturvedi, Vinita,Manju,Sinha, Sudhir
scheme or table, p. 1121 - 1127 (2009/12/26)
Aryl and heteroaryl derivatives with an alkylaminoethyl chain on the hydroxyl group of the benzene ring are prepared and evaluated against Mycobacterium tuberculosis H37RV and showed the activity in the range of 3.12-25 μg/mL. The compounds containing alkylaminoethyl chains on aryl-chromeneyl carbinol do not show good activity. Similarly compounds with bis and tris-alkylaminoethyl chains on aryl and triarylmethane derivatives do not exhibit antitubcrcular activity. Among heteroaryl containing triarylmcthanes (TRAMs), thiophene derivatives with alkylaminoethyl chain on aromatic hydroxyl group have exhibited good antitubercular activity. On the other hand, pyrrole containing TRAMs do not show good activity.
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation
De Martino, Gabriella,Regina, Giuseppe La,Pasquali, Alessandra Di,Ragno, Rino,Bergamini, Alberto,Ciaprini, Chiara,Sinistro, Anna,Maga, Giovanni,Crespan, Emmanuele,Artico, Marino,Silvestri, Romano
, p. 4378 - 4388 (2007/10/03)
1-[2-(Diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles (DAMNIs) is a novel family of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) active at submicromolar concentration. Replacement of one phenyl ring of 1-[2-(diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole (4) with heterocyclic rings, such as 2-thienyl or 3-pyridinyl, led to novel DAMNIs with increased activity. In HIV-1 WT cell-based assay the racemic 1-{2-[α-(thiophen-2-yl) phenylmethoxy]ethyl}-2-methyl-5-nitroimidazole (7) (EC50 = 0.03 μM) proved 5 times more active than compound 4. Docking experiments showed that the introduction of a chiral center would not affect the binding of both (R)-7 and (S)-7. The internal scoring function of the Autodock program calculated the same inhibition constant (Ki = 7.9 nM) for the two enantiomers. Compounds 7 (ID50 = 8.25 μM) were found more active than efavirenz (ID50 = 25 μM) against the viral RT carrying the K103N mutation, suggesting for these compounds a potential use in efavirenz based anti-AIDS regimens.