title: Microwave-assisted combinatorial synthesis of 2-alkyl-2-(N-arylsulfonylindol- 3-yl)-3-N-Acyl-5-Aryl-1,3,4-oxadiazolines as anti-HIV-1 agents.
abstract: A library of new 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines was efficiently synthesized from hydrazones and anhydrides under microwave irradiation and solvent-free conditions. Compared with the traditional procedure (100 equiv. of anhydride and 1.5-4 h of reaction time), the present methodology has the advantages of short reaction time (10-20 min), and avoiding excess of anhydride (only 1.5 equiv.). Moreover, two compounds exhibited the promising anti-HIV-1 activity when evaluated for their inhibitory activity against HIV-1 replication in acutely infected C8166 cells.
authors.affiliation: Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China.
authors.forename: Zhi-Ping
authors.initials: ZP
authors.lastname: Che
authors.forename: Ning
authors.initials: N
authors.lastname: Huang
authors.forename: Xiang
authors.initials: X
authors.lastname: Yu
authors.forename: Liu-Meng
authors.initials: LM
authors.lastname: Yang
authors.forename: Jun-Qiang
authors.initials: JQ
authors.lastname: Ran
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Zhi
authors.forename: Hui
authors.initials: H
authors.lastname: Xu
authors.forename: Yong-Tang
authors.initials: YT
authors.lastname: Zheng
mesh_terms: D000812:Anhydrides / Q000737:chemistry; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D006835:Hydrazones / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure; D010069:Oxadiazoles / Q000737:chemistry*; D013997:Time Factors; D015215:Zidovudine / Q000494:pharmacology
chemical_list: D000812:Anhydrides; D019380:Anti-HIV Agents; D006835:Hydrazones; D010069:Oxadiazoles; D015215:Zidovudine