266 research outputs found

    Larvicidal activities of 2-Aryl-2,3-Dihydroquinazolin -4-ones against malaria vector Anopheles arabiensis, In Silico ADMET prediction and molecular target investigation

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    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.Fil: Venugopala, K. N.. Durban University Of Technology; SudĂĄfricaFil: Pushpalatha, R.. Reva University; IndiaFil: Tratat, C.. King Faisal University; Arabia SauditaFil: Gleiser, Raquel M.. Consejo Nacional de Investigaciones CientĂ­ficas y TĂ©cnicas. Centro CientĂ­fico TecnolĂłgico CĂłrdoba. Instituto Multidisciplinar de BiologĂ­a Vegetal (P). Grupo Vinculado Centro de Relevamiento y EvaluaciĂłn de Recursos AgrĂ­colas y Naturales; ArgentinaFil: Bhandary, S.. Indian Institute Of Science Education And Research Bhopal; IndiaFil: Chopra, D.. Indian Institute Of Science Education And Research Bhopal; IndiaFil: Morsy, M.. King Faisal University; Arabia SauditaFil: Al-Dhubiab, B. E.. King Faisal University; Arabia SauditaFil: Attimarad, M. B.. King Faisal University; Arabia SauditaFil: Nair, A.. King Faisal University; Arabia SauditaFil: Sreeharsha, N.. King Faisal University; Arabia SauditaFil: Venugopala, R.. University Of Kwazulu-natal; SudĂĄfricaFil: Deb, P. K.. Philadelphia University; JordaniaFil: Chandrashekharappa, S.. Institute For Stem Cell Biology And Regenerative Medicine; IndiaFil: Khalil, H.. King Faisal University; Arabia SauditaFil: Alwassil, O.. King Saud Bin Abdulaziz University For Health Sciences; Arabia SauditaFil: Abed, S. N.. Philadelphia University; JordaniaFil: Bataineh, Y. A.. Philadelphia University; JordaniaFil: Palenge, R.. Reva University; IndiaFil: Haroun, M.. King Faisal University; Arabia SauditaFil: Pottathil, S.. King Faisal University; Arabia SauditaFil: Girish, M. B.. Reva University; IndiaFil: Akrawi, S. H.. King Faisal University; Arabia SauditaFil: Mohanlall, V.. Durban University Of Technology; SudĂĄfric

    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

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    Alteration of insect growth regulators by the action of inhibitors is becoming an attractive strategy to combat disease-transmitting insects. In the present study, we investigated the larvicidal effect of 1,2,3-triazolyl-pyrimidinone derivatives against the larvae of the mosquito Anopheles arabiensis, a vector of malaria. All compounds demonstrated insecticidal activity against mosquito larvae in a dose-dependent fashion. A preliminary study of the structure–activity relationship indicated that the electron-withdrawing substituent in the para position of the 4-phenyl-pyrimidinone moiety enhanced the molecules’ potency. A docking study of these derivatives revealed favorable binding affinity for the sterol carrier protein-2 receptor, a protein present in the intestine of the mosquito larvae. Being effective insecticides against the malaria-transmitting Anopheles arabiensis, 1,2,3-triazole-based pyrimidinones represent a starting point to develop novel inhibitors of insect growth regulators.Fil: Venugopala, Katharigatta N.. Durban University Of Technology; SudĂĄfrica. King Faisal University; Arabia SauditaFil: Shinu, Pottathil. King Faisal University; Arabia SauditaFil: Tratrat, Christophe. King Faisal University; Arabia SauditaFil: Deb, Pran Kishore. Philadelphia University Jordan; JordaniaFil: Gleiser, Raquel M.. Universidad Nacional de CĂłrdoba; Argentina. Consejo Nacional de Investigaciones CientĂ­ficas y TĂ©cnicas. Centro CientĂ­fico TecnolĂłgico CĂłrdoba. Instituto Multidisciplinar de BiologĂ­a Vegetal (P). Grupo Vinculado Centro de Relevamiento y EvaluaciĂłn de Recursos AgrĂ­colas y Naturales; ArgentinaFil: Chandrashekharappa, Sandeep. National Institute Of Pharmaceutical Education And Research, Raebareli; IndiaFil: Chopra, Deepak. Indian Institute Of Science Education And Research Bhopal; IndiaFil: Attimarad, Mahesh. King Faisal University; Arabia SauditaFil: Nair, Anroop B.. King Faisal University; Arabia SauditaFil: Sreeharsha, Nagaraja. Vidya Siri College Of Pharmacy; India. King Faisal University; Arabia SauditaFil: Mahomoodally, Fawzi M.. University Of Mauritius; MauricioFil: Haroun, Michelyne. King Faisal University; Arabia SauditaFil: Kandeel, Mahmoud. Faculty Of Veteinary Medicine; Egipto. King Faisal University; Arabia SauditaFil: Asdaq, Syed Mohammed Basheeruddin. Almaarefa University; Arabia SauditaFil: Mohanlall, Viresh. Durban University Of Technology; SudĂĄfricaFil: Al-Shari, Nizar A.. Jordan University Of Science And Technology; JordaniaFil: Morsy, Mohamed A.. King Faisal University; Arabia Saudita. Faculty Of Medicine; Egipt

    Increased incidence of kidney diseases in general practice after a nationwide albuminuria self-test program

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    <p>Abstract</p> <p>Background</p> <p>To study the influence of a nationwide albuminuria self-test program on the number of GP contacts for urinary complaints and/or kidney diseases and the number of newly diagnosed patients with kidney diseases by the GP.</p> <p>Methods</p> <p>Data were used from the Netherlands Information Network of General Practice (LINH), including a representative sample of general practices with a dynamic population of approximately 300.000 listed patients. Morbidity data were retrieved from electronic medical records, kept in a representative sample of general practices. The incidence of kidney diseases and urinary complaints before and after the albuminuria self-test program was compared with logistic regression analyses.</p> <p>Results</p> <p>Data were used from 139 general practices, including 444,220 registered patients. The number of GP consultations for kidney diseases and urinary complaints was increased in the year after the albuminuria self-test program and particularly shortly after the start of the program. Compared with the period before the self-test program, more patients have been diagnosed by the GP with symptoms/complaints of kidney disease and urinary diseases (OR = 1.7 (CI 1.4 - 2.0) and OR = 2.1 (CI 1.9 - 2.3), respectively). The odds on an abnormal urine-test in the period after the self-test program was three times higher than the year before (OR = 3.0 (CI 2.4 - 3.6)). The effect of the self-test program on newly diagnosed patients with an abnormal urine test was modified by both the presence of the risk factors hypertension and diabetes mellitus. For this diagnosis the highest OR was found in patients without both conditions (OR = 4.2 (CI 3.3 - 5.4)).</p> <p>Conclusions</p> <p>A nationwide albuminuria self-test program resulted in an increasing number of newly diagnosed kidney complaints and diseases the year after the program. The highest risks were found in patients without risk factors for kidney diseases.</p

    Registration of cancer in girls remains lower than expected in countries with low/middle incomes and low female education rates.

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    BACKGROUND: A decade ago it was reported that childhood cancer incidence was higher in boys than girls in many countries, particularly those with low gross domestic product (GDP) and high infant mortality rate. Research suggests that socio-economic and cultural factors are likely to be responsible. This study aimed to investigate the association between cancer registration rate sex ratios and economic, social and healthcare-related factors using recent data (1998-2002). METHODS: For 62 countries, childhood (0-15 years) cancer registration rate sex ratios were calculated from Cancer Incidence in Five Continents Vol IX, and economic, social and healthcare indicator data were collated. RESULTS: Increased age standardised cancer registration rate sex ratio (M:F) was significantly associated with decreasing life expectancy (P=0.05), physician density (P=0.05), per capita health expenditure (P=0.05), GDP (P=0.01), education sex ratios (primary school enrolment sex ratio (P<0.01); secondary school enrolment sex ratio (P<0.01); adult literacy sex ratio (P<0.01)) and increasing proportion living on less than Int$1 per day (P=0.03). CONCLUSION: The previously described cancer registration sex disparity remains, particularly, in countries with poor health system indicators and low female education rates. We suggest that girls with cancer continue to go undiagnosed and that incidence data, particularly in low- and middle-income countries, should continue to be interpreted with caution
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