- Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria
-
A series of N-phenyl-2,5-dimethylpyrrole derivatives, designed as hybrids of the antitubercular agents BM212 and SQ109, have been synthesized and evaluated against susceptible and drug-resistant mycobacteria strains. Compound 5d, bearing a cyclohexylmethylene side chain, showed high potency against M. tuberculosis including MDR-TB strains at submicromolar concentrations. The new compound shows bacteriostatic activity and low toxicity and proved to be effective against intracellular mycobacteria too, showing an activity profile similar to isoniazid.
- Touitou, Meir,Manetti, Fabrizio,Ribeiro, Camila Maringolo,Pavan, Fernando Rogerio,Scalacci, Nicolò,Zrebna, Katarina,Begum, Neelu,Semenya, Dorothy,Gupta, Antima,Bhakta, Sanjib,Mchugh, Timothy D.,Senderowitz, Hanoch,Kyriazi, Melina,Castagnolo, Daniele
-
supporting information
p. 638 - 644
(2020/01/11)
-
- Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors
-
A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.
- Feng, Song,Hong, Di,Wang, Baoxia,Zheng, Xiufang,Miao, Kun,Wang, Lisha,Yun, Hongying,Gao, Lu,Zhao, Shuhai,Shen, Hong C.
-
supporting information
p. 359 - 362
(2015/03/30)
-
- SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
-
The present invention provides fused derivatives of Formula (I) that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PBKs including, for example, inflammatory disorders, immune- based disorders, cancer, and other diseases.
- -
-
Page/Page column 57
(2011/07/07)
-
- IMIDAZO[1,2-A]PYRIDINES FOR THE TREATMENT OF CNS AND CARDIAC DISEASES
-
The present invention relates to imidazo[1,2-a]pyridine compounds of formula (1) STR1 which are dopamine D-4 antagonists and useful as anti-psychotic agents.
- -
-
-
