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Research Publications (Applied Sciences)

Permanent URI for this collectionhttp://ir-dev.dut.ac.za/handle/10321/213

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Author: search.filters.author.Gleiser, Raquel M.Has files: Yes

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    Larvicidal Activities of 2-Aryl-2,3-Dihydroquinazolin-4-ones against Malaria Vector Anopheles arabiensis, in Silico ADMET prediction and molecular target investigation
    (MDPI, 2020-03-02) Venugopala, Katharigatta Narayanaswamy; Ramachandra, Pushpalatha; Tratrat, Christophe; Gleiser, Raquel M.; Bhandary, Subhrajyoti; Chopra, Deepak; Morsy, Mohamed A.; Aldhubiab, Bandar E.; Attimarad, Mahesh; Nair, Anroop B.; Sreeharsha, Nagaraja; Venugopala, Rashmi; Deb, Pran Kishore; Chandrashekharappa, Sandeep; Khalil, Hany Ezzat; Alwassil, Osama I.; Abed, Sara Nidal; Bataineh, Yazan A.; Palenge, Ramachandra; Haroun, Michelyne; Pottathil, Shinu; Girish, Meravanige B.; Akrawi, Sabah H.; Mohanlall, Viresh
    Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through the bites of infected Anopheles mosquitoes. Although insecticides are currently used to reduce malaria transmission, their safety concern for living systems, as well as the environment, is a growing problem. Therefore, the discovery of novel, less toxic, and environmentally safe molecules to effectively combat the control of these vectors is in high demand. In order to identify new potential larvicidal agents, a series of 2-aryl-1,2-dihydroquinazolin-4-one derivatives were synthesized and evaluated for their larvicidal activity against Anopheles arabiensis. The in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the compounds were also investigated and most of the derivatives possessed a favorable ADMET profile. Computational modeling studies of the title compounds demonstrated a favorable binding interaction against the acetylcholinesterase enzyme molecular target. Thus, 2-aryl-1,2-dihydroquinazolin-4-ones were identified as a novel class of Anopheles arabiensis insecticides which can be used as lead molecules for the further development of more potent and safer larvicidal agents for treating malaria.
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    Antimosquito properties of 2-substituted phenyl/benzylamino-6-(4-chlorophenyl)-5-methoxycarbonyl-4-methyl-3,6-dihydropyrimidin-1-ium chlorides against anopheles arabiensis
    (Bentham Science Publishers, 2014) Gleiser, Raquel M.; Chalannavar, Raju K.; Odhav, Bharti; Odhav, Bharti; Venugopala, Katharigatta Narayanaswamy
    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 arabien-sis. 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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    The antimosquito properties of extracts from flowering plants in South Africa
    (NCBI, 2013) Chalannavar, Raju K.; Hurinanthan, Vashka; Singh, Alveera; Venugopala, Katharigatta Narayanaswamy; Gleiser, Raquel M.; Baijnath, Himansu; Odhav, Bharti
    Extracts of selected flowering plants, which are considered eco-friendly, are used for the treatment of numerous ailments and vector control worldwide. This has resulted in approximately 25 per cent of currently used drugs being derived from herbal sources. The aqueous and methanolic extracts of twelve plant species, Psidium guajava (pink fruit), Psidium guajava (white fruit), Psidium cattleianum var. cattleianum, Psidium guineense and Psidium X durbanensis, Achyranthes aspera, Alternanthera sessilis, Guilleminea densa, Capparis tomentosa, Leonotis leonurus, Dichrostachys cinerea and Carpobrotus dimidiatus, were tested for insecticidal activity, including larvicidal, adulticidal and repellent activities against the adult female mosquito, Anopheles arabiensis. The extracts of P. guajava (white fruit), C. tomentosa, L. leonurus,D. cinerea, and C. dimidiatus exerted a pronounced inhibitory effect on adult insects, while those of P. guajava (pink fruit), P. X durbanensis, P. cattleianum var. cattleianum, P. guineense, A. aspera, A. sessilis, and G. densa were ineffective and failed to satisfy the criteria set by the World Health Organization. In the tests for repellency against An. arabiensis, all the tested aqueous and methanolic plant extracts except those of A. sessilis repelled 80-100% of mosquitoes. The most effective mosquito repellents were the methanol and aqueous extracts of P. guajava (pink fruit), P. X durbanensis, P. cattleianum var. cattleianum, P. guineense, G. densa,L. leonurus and D. cinerea, which are potential sources of cost effective mosquito repellents to be utilized in malarial endemic areas.