Syntheses of new substituted triazino tetrahydroisoquinolines and beta-carbolines as novel antileishmanial agents.
A series of triazino tetrahydroisoquinolines (3-5) and beta-carboline derivatives (15-27) have been synthesized as novel antileishmanial agents. Among them, compounds 15, 16 and 25 have shown 78.0%, 78.6% and 68.0% in vivo inhibition against Leishmania donovani at a dose of 50 mg kg(-1) x 5 days, respectively, while compounds 3 and 18 exhibited 55.6% and 53.3% in vivo inhibitions, respectively, against L. donovani at a dose of 50 mg kg(-1) x 5 days.
Kumar
Arun
A
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Katiyar
Sanjay Babu
SB
Gupta
Suman
S
Chauhan
Prem M S
PM
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D008647:Mesocricetus; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014227:Triazines / Q000737:chemistry*
D000981:Antiprotozoal Agents; D002243:Carbolines; D044005:Tetrahydroisoquinolines; D014227:Triazines