Literature DB >> 24506684

Antimosquito properties of 2-substituted phenyl/benzylamino-6-(4-chlorophenyl)-5-methoxycarbonyl-4-methyl-3,6-dihydropyrimidin--ium chlorides against Anopheles arabiensis.

Venugopala K Narayanaswamy, Raquel M Gleiser, Raju K Chalannavar, Bharti Odhav1.   

Abstract

Eight novel dihydropyrimidine analogs named DHPM1-DHPM8 was synthesized in their hydrochloride salt form using one pot synthesis between methyl 2-chloro-4-(4-chlorophenyl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate and substituted arylamines in isopropanol. The antimosquito effect of the test compounds were assessed against the adult mosquito Anopheles arabiensis. For adulticidal properties the test compounds were sprayed onto ceramic tiles and screened using the cone bio-assay method. The larvicidal activity was tested by monitoring larval mortality daily and up to 3 days of exposure. Repellency properties were tested in a feeding-probe assay using unfed female Anopheles arabiensis. Compounds DHPM1, DHPM4, DHPM5 and DHPM6 exerted larval mortality equivalent to temephos (trade name Abate, a commercial larvicidal compound). Compounds DHPM1 to DHPM5 repelled or knocked down 92 to 98% of mosquitoes exposed to rodent skin treated with the compounds. None of the compounds showed any significant activity against the adult mosquito Anopheles arabiensis.

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Year:  2014        PMID: 24506684     DOI: 10.2174/157340641002140131164945

Source DB:  PubMed          Journal:  Med Chem        ISSN: 1573-4064            Impact factor:   2.745


  7 in total

1.  Novel dihydropyrimidine derivatives as potential HDAC inhibitors: in silico study.

Authors:  Ganapathi Thipparapu; Rajanna Ajumeera; Vijayalakshmi Venkatesan
Journal:  In Silico Pharmacol       Date:  2017-10-12

2.  1,2,3-Triazolyl-tetrahydropyrimidine Conjugates as Potential Sterol Carrier Protein-2 Inhibitors: Larvicidal Activity against the Malaria Vector Anopheles arabiensis and In Silico Molecular Docking Study.

Authors:  Katharigatta N Venugopala; Pottathil Shinu; Christophe Tratrat; Pran Kishore Deb; Raquel M Gleiser; Sandeep Chandrashekharappa; Deepak Chopra; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Fawzi M Mahomoodally; Michelyne Haroun; Mahmoud Kandeel; Syed Mohammed Basheeruddin Asdaq; Viresh Mohanlall; Nizar A Al-Shar'i; Mohamed A Morsy
Journal:  Molecules       Date:  2022-04-21       Impact factor: 4.927

3.  Evaluation of halogenated coumarins for antimosquito properties.

Authors:  Venugopala K Narayanaswamy; Raquel M Gleiser; Kabange Kasumbwe; Bandar E Aldhubiab; Mahesh V Attimarad; Bharti Odhav
Journal:  ScientificWorldJournal       Date:  2014-12-25

4.  Design, synthesis, and characterization of (1-(4-aryl)- 1H-1,2,3-triazol-4-yl)methyl, substituted phenyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates against Mycobacterium tuberculosis.

Authors:  Katharigatta N Venugopala; G B Dharma Rao; Subhrajyoti Bhandary; Melendhran Pillay; Deepak Chopra; Bandar E Aldhubiab; Mahesh Attimarad; Osama Ibrahim Alwassil; Sree Harsha; Koleka Mlisana
Journal:  Drug Des Devel Ther       Date:  2016-08-25       Impact factor: 4.162

5.  Synthesis and cytotoxic effect of a few N-heteroaryl enamino amides and dihydropyrimidinethiones on AGS and MCF-7 human cancer cell lines.

Authors:  Sajjad Tavangar; Shahab Bohlooli; Nima Razzaghi-Asl
Journal:  Res Pharm Sci       Date:  2020-05-11

6.  Larvicidal Activities of 2-Aryl-2,3-Dihydroquinazolin -4-ones against Malaria Vector Anopheles arabiensis, In Silico ADMET Prediction and Molecular Target Investigation.

Authors:  Katharigatta N Venugopala; Pushpalatha Ramachandra; Christophe Tratrat; Raquel M Gleiser; Subhrajyoti Bhandary; Deepak Chopra; Mohamed A Morsy; Bandar E Aldhubiab; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Pran Kishore Deb; Sandeep Chandrashekharappa; Hany Ezzat Khalil; Osama I Alwassil; Sara Nidal Abed; Yazan A Bataineh; Ramachandra Palenge; Michelyne Haroun; Shinu Pottathil; Meravanige B Girish; Sabah H Akrawi; Viresh Mohanlall
Journal:  Molecules       Date:  2020-03-13       Impact factor: 4.411

7.  In silico Design and Synthesis of Tetrahydropyrimidinones and Tetrahydropyrimidinethiones as Potential Thymidylate Kinase Inhibitors Exerting Anti-TB Activity Against Mycobacterium tuberculosis.

Authors:  Katharigatta N Venugopala; Christophe Tratrat; Melendhran Pillay; Sandeep Chandrashekharappa; Omar Husham Ahmed Al-Attraqchi; Bandar E Aldhubiab; Mahesh Attimarad; Osama I Alwassil; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Mohamed A Morsy; Michelyne Haroun; Hezekiel M Kumalo; Bharti Odhav; Koleka Mlisana
Journal:  Drug Des Devel Ther       Date:  2020-03-09       Impact factor: 4.162

  7 in total

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