title: One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents.
abstract: An efficient one pot synthesis of a series of pluripotent (E)-1-(3-methyl-5-aryl-7-styryl-5H-thiazolo[3,2-a]pyrimidin-6-yl)-3-arylprop-2-en-1-ones is reported. It involves reaction of 5-acetyl-6-methyl-4-aryl-dihydropyrimidine-2-thiones, propargyl bromide and aromatic aldehydes in presence of ethanolic KOH. The newly synthesized compounds were evaluated for antimalarial activity against Plasmodium falciparum and as HIV-RT inhibitors. Most of the compound displayed potent antimalarial activity with IC(50)<2 μg/mL. Compounds 6, 11 and 20 showed better activity against P. falciparum K1 strains in comparison to standard drug chloroquine. Compounds 6, 11, and 16 exhibited 73.44, 66.92, and 70.81% HIV-RT inhibition at 100 μg/mL.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, India.
authors.forename: Seerat
authors.initials: S
authors.lastname: Fatima
authors.forename: Anindra
authors.initials: A
authors.lastname: Sharma
authors.forename: Reshu
authors.initials: R
authors.lastname: Saxena
authors.forename: Rajkamal
authors.initials: R
authors.lastname: Tripathi
authors.forename: Sanjeev K
authors.initials: SK
authors.lastname: Shukla
authors.forename: Swaroop Kumar
authors.initials: SK
authors.lastname: Pandey
authors.forename: Renu
authors.initials: R
authors.lastname: Tripathi
authors.forename: Rama P
authors.initials: RP
authors.lastname: Tripathi
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D002522:Chlorocebus aethiops; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D020128:Inhibitory Concentration 50; D010963:Plasmodium falciparum / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D014709:Vero Cells
chemical_list: D019380:Anti-HIV Agents; D000962:Antimalarials; D011743:Pyrimidines; D054303:HIV Reverse Transcriptase