Synthesis and antitubercular activity of substituted phenylmethyl- and pyridylmethyl amines.
A total of 42 benzyl- and pyridylmethyl amines were synthesized either by reductive amination of aromatic/heteroaromatic aldehydes with amines or by conjugate addition of amines to the cinnamates followed by reduction of the ester group with lithium aluminium hydride to the respective propanolamines. All the synthesized compounds were evaluated against both avirulent and virulent strains of Mycobacterium tuberculosis. Many of the compounds exhibited MIC as low as 1.56microg/mL. Few of potent compounds were also evaluated against clinical isolates of MDR TB and found to be active at one or other concentrations with MIC as low as 3.12microg/mL.
Tripathi
R P
RP
Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. rpt_56@yahoo.com
Saxena
Nisha
N
Tiwari
V K
VK
Verma
S S
SS
Chaturvedi
Vinita
V
Manju
Y K
YK
Srivastva
A K
AK
Gaikwad
A
A
Sinha
S
S
D000588:Amines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D024901:Drug Resistance, Multiple, Bacterial; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000145:classification / Q000187:drug effects*
D000588:Amines; D000995:Antitubercular Agents