Research Publications (Applied Sciences)
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Item 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, VireshMalaria, 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.Item Synthesis, polymorphism, and insecticidal activity of Methyl 4-(4-chlorophenyl)-8-iodo-2-methyl-6-oxo-1,6-dihydro-4H-pyrimido[2,1-b]quinazoline-3-Carboxylate against Anopheles arabiensis mosquito.(Wiley Online Library, 2016-07) Venugopala, Katharigatta Narayanaswamy; Nayak, Susanta K.; Gleiser, Raquel M.; Sanchez-Borzone, M. E.; Garcia, D. A.; Odhav, BhartiMosquitoes are the major vectors of pathogens and parasites including those causing malaria, the most deadly vector-borne disease. The negative environmental effects of most synthetic compounds combined with widespread development of insecticide resistance encourage an interest in finding and developing alternative products against mosquitoes. In this study, pyrimido[2,1-b]quinazoline derivative DHPM3 has been synthesized by three-step chemical reaction and screened for larvicide, adulticide, and repellent properties against Anopheles arabiensis, one of the dominant vectors of malaria in Africa. The title compound emerged as potential larvicide agent for further research and development, because it exerted 100% mortality, while adulticide activity was considered moderate.Item 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 NarayanaswamyEight 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.Item 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, BhartiExtracts 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.Item Synthesis and antimosquito properties of 2,6-substituted benzo[ d ] thiazole and 2,4-substituted benzo[ d ]thiazole analogues against Anopheles arabiensis(Elsevier, 2013-07) Venugopala, Katharigatta Narayanaswamy; Krishnappa, Krishnappa; Nayak, Susanta K.; Subrahmanya, Bhat K.; Vaderapura, Jayashankaragowda P.; Chalannavar, Raju K.; Gleiser, Raquel M.; Odhav, BhartiA novel and efficient one pot synthesis was developed for 2,6-substituted-benzo[d]thiazole analogues 4a–k and 2,4-substituted-benzo[d]thiazole analogues 4l–pvia three component condensation reaction of substituted arylaldehyde, 2-amino-6-halo/4-methyl-benzo[d]thiazole and 2-naphthol or 6-hydroxyquinoline in presence of 10% w/v NaCl in water by microwave method. This method enabled for short reaction times, easy work-up and significant high yields. The title compound 4b was used for single crystal X-ray studies in order to understand its conformation and packing features. The title compounds 4a–p were screened for antimosquito properties such as repellency, insecticidal and larvicidal activity against Anopheles arabiensis by mosquito feeding-probing assay, cone bio-assay and standard WHO larvicidal assay, respectively. Among these analogous 4b, 4d and 4p exhibit the highest repellent activity comparable to the positive control DEET, and 4a and 4k knockdown most mosquitoes on repellent assays.