Literature DB >> 22871486

One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents.

Seerat Fatima1, Anindra Sharma, Reshu Saxena, Rajkamal Tripathi, Sanjeev K Shukla, Swaroop Kumar Pandey, Renu Tripathi, Rama P Tripathi.   

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.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2012        PMID： 22871486     DOI： 10.1016/j.ejmech.2012.07.018

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  6 in total

Review 1.  Targeting endosomal acidification by chloroquine analogs as a promising strategy for the treatment of emerging viral diseases.

Authors:  Md Abdul Alim Al-Bari
Journal:  Pharmacol Res Perspect       Date:  2017-01-23

2.  Promising Antidiabetic and Antimicrobial Agents Based on Fused Pyrimidine Derivatives: Molecular Modeling and Biological Evaluation with Histopathological Effect.

Authors:  Fatma Bassyouni; Mohammad Tarek; Abeer Salama; Bassant Ibrahim; Sawsan Salah El Dine; Nemat Yassin; Amina Hassanein; Maysa Moharam; Mohamed Abdel-Rehim
Journal:  Molecules       Date:  2021-04-19       Impact factor: 4.411

3.  Synthesis, crystal structure and antibacterial studies of dihydropyrimidines and their regioselectively oxidized products.

Authors:  Alakbar E Huseynzada; Christian Jelch; Haji Vahid N Akhundzada; Sarra Soudani; Cherif Ben Nasr; Aygun Israyilova; Filippo Doria; Ulviyya A Hasanova; Rana F Khankishiyeva; Mauro Freccero
Journal:  RSC Adv       Date:  2021-02-03       Impact factor: 3.361

4.  Biomimetic hydrogenation of electron deficient olefins using in situ generated 2-arylbenzimidazoline: synthesis of novel 3-benzylbenzo[4,5]thiazolo[3,2-a]pyrimidin-4-ones.

Authors:  Maryam Danehchin; Abbas Ali Esmaeili
Journal:  Mol Divers       Date:  2021-06-11       Impact factor: 2.943

5.  Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues.

Authors:  Ebtesam A Basiony; Allam A Hassan; Zahra M Al-Amshany; Ahmed A Abd-Rabou; Adel A-H Abdel-Rahman; Nasser A Hassan; Wael A El-Sayed
Journal:  Molecules       Date:  2020-01-18       Impact factor: 4.411

6.  Identification of 3-((1-(Benzyl(2-hydroxy-2-phenylethyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamoyl)pyrazine-2-carboxylic Acid as a Potential Inhibitor of Non-Nucleosidase Reverse Transcriptase Inhibitors through InSilico Ligand- and Structure-Based Approaches.

Authors:  Deepti Mathpal; Tahani M Almeleebia; Kholoud M Alshahrani; Mohammad Y Alshahrani; Irfan Ahmad; Mohammed Asiri; Mehnaz Kamal; Talha Jawaid; Swayam Prakash Srivastava; Mohd Saeed; Vishal M Balaramnavar
Journal:  Molecules       Date:  2021-08-30       Impact factor: 4.411
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.