Synthesis of galactopyranosyl amino alcohols as a new class of antitubercular and antifungal agents.
The galactopyranosyl amino alcohols (3-16) were synthesised by regioselective oxirane ring opening of compound 2 with variety of amines and screened for antitubercular and antifungal activities. One of the compounds (16) showed potent activity against Mycobacterium tuberculosis H37 Rv in vitro and also displayed activity in MDR TB. The compound (16) was found to be superior to ethambutol clinically used anti TB drug in in vitro screen.
Tewari
Neetu
N
Division of Medicinal Chemistry, Central Drug Research Institute, -226001, Lucknow, India.
Tiwari
V K
VK
Tripathi
R P
RP
Chaturvedi
V
V
Srivastava
A
A
Srivastava
R
R
Shukla
P K
PK
Chaturvedi
A K
AK
Gaikwad
A
A
Sinha
S
S
Srivastava
B S
BS
D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005690:Galactose / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000254:growth & development
D000605:Amino Alcohols; D000935:Antifungal Agents; D000995:Antitubercular Agents; D005690:Galactose