1,2,3-Triazolyl-tetrahydropyrimidine conjugates as potential Sterol Carrier Protein-2 Inhibitors: Larvicidal activity against the Malaria Vector Anopheles arabiensis and In Silico...

Autores: Venugopala, Katharigatta N.; Shinu, Pottathil; Tratrat, Christophe; Deb, Pran Kishore; Gleiser, Raquel M.; Chandrashekharappa, Sandeep; Chopra, Deepak; Attimarad, Mahesh; Nair, Anroop B.; Sreeharsha, Nagaraja; Mahomoodally, Fawzi M.; Haroun, Michelyne; Kandeel, Mahmoud; Asdaq, Syed Mohammed Basheeruddin; Mohanlall, Viresh; Al-Shari, Nizar A.; Morsy, Mohamed A.
Año de publicación: 2022
Idioma: inglés
Tipo de recurso: artículo
Estado: versión publicada
Descripción: 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; Sudáfrica. King Faisal University; Arabia Saudita
Fil: Shinu, Pottathil. King Faisal University; Arabia Saudita
Fil: Tratrat, Christophe. King Faisal University; Arabia Saudita
Fil: Deb, Pran Kishore. Philadelphia University Jordan; Jordania
Fil: Gleiser, Raquel M.. Universidad Nacional de Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinar de Biología Vegetal (P). Grupo Vinculado Centro de Relevamiento y Evaluación de Recursos Agrícolas y Naturales; Argentina
Fil: Chandrashekharappa, Sandeep. National Institute Of Pharmaceutical Education And Research, Raebareli; India
Fil: Chopra, Deepak. Indian Institute Of Science Education And Research Bhopal; India
Fil: Attimarad, Mahesh. King Faisal University; Arabia Saudita
Fil: Nair, Anroop B.. King Faisal University; Arabia Saudita
Fil: Sreeharsha, Nagaraja. Vidya Siri College Of Pharmacy; India. King Faisal University; Arabia Saudita
Fil: Mahomoodally, Fawzi M.. University Of Mauritius; Mauricio
Fil: Haroun, Michelyne. King Faisal University; Arabia Saudita
Fil: Kandeel, Mahmoud. Faculty Of Veteinary Medicine; Egipto. King Faisal University; Arabia Saudita
Fil: Asdaq, Syed Mohammed Basheeruddin. Almaarefa University; Arabia Saudita
Fil: Mohanlall, Viresh. Durban University Of Technology; Sudáfrica
Fil: Al-Shari, Nizar A.. Jordan University Of Science And Technology; Jordania
Fil: Morsy, Mohamed A.. King Faisal University; Arabia Saudita. Faculty Of Medicine; Egipto
Materia: ANOPHELES ARABIENSIS
BIGINELLI REACTION
CLICK CHEMISTRY
IN SILICO DOCKING
MOLECULAR HYBRIDIZATION
MOSQUITO LARVICIDAL ACTIVITY
PYRIMIDINE
STEROL CARRIER PROTEIN-2
TRIAZOLE
Nivel de accesibilidad: acceso abierto
Condiciones de uso: https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
Institución: Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador: oai:ri.conicet.gov.ar:11336/200568

Acceder

id	CONICETDig_d00203a6e88025f2d97eecfbebd0b767
oai_identifier_str	oai:ri.conicet.gov.ar:11336/200568
network_acronym_str	CONICETDig
repository_id_str	3498
network_name_str	CONICET Digital (CONICET)
spelling	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 StudyVenugopala, Katharigatta N.Shinu, PottathilTratrat, ChristopheDeb, Pran KishoreGleiser, Raquel M.Chandrashekharappa, SandeepChopra, DeepakAttimarad, MaheshNair, Anroop B.Sreeharsha, NagarajaMahomoodally, Fawzi M.Haroun, MichelyneKandeel, MahmoudAsdaq, Syed Mohammed BasheeruddinMohanlall, VireshAl-Shari, Nizar A.Morsy, Mohamed A.ANOPHELES ARABIENSISBIGINELLI REACTIONCLICK CHEMISTRYIN SILICO DOCKINGMOLECULAR HYBRIDIZATIONMOSQUITO LARVICIDAL ACTIVITYPYRIMIDINESTEROL CARRIER PROTEIN-2TRIAZOLEhttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Alteration 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; Sudáfrica. 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 Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinar de Biología Vegetal (P). Grupo Vinculado Centro de Relevamiento y Evaluación de Recursos Agrícolas 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; SudáfricaFil: Al-Shari, Nizar A.. Jordan University Of Science And Technology; JordaniaFil: Morsy, Mohamed A.. King Faisal University; Arabia Saudita. Faculty Of Medicine; EgiptoMolecular Diversity Preservation International2022-05info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/200568Venugopala, Katharigatta N.; Shinu, Pottathil; Tratrat, Christophe; Deb, Pran Kishore; Gleiser, Raquel M.; et al.; 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; Molecular Diversity Preservation International; Molecules; 27; 9; 5-2022; 1-161420-3049CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.3390/molecules27092676info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/1420-3049/27/9/2676info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:09:10Zoai:ri.conicet.gov.ar:11336/200568instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:09:11.229CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv	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
title	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
spellingShingle	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 Venugopala, Katharigatta N. ANOPHELES ARABIENSIS BIGINELLI REACTION CLICK CHEMISTRY IN SILICO DOCKING MOLECULAR HYBRIDIZATION MOSQUITO LARVICIDAL ACTIVITY PYRIMIDINE STEROL CARRIER PROTEIN-2 TRIAZOLE
title_short	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
title_full	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
title_fullStr	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
title_full_unstemmed	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
title_sort	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
dc.creator.none.fl_str_mv	Venugopala, Katharigatta N. Shinu, Pottathil Tratrat, Christophe Deb, Pran Kishore Gleiser, Raquel M. Chandrashekharappa, Sandeep Chopra, Deepak Attimarad, Mahesh Nair, Anroop B. Sreeharsha, Nagaraja Mahomoodally, Fawzi M. Haroun, Michelyne Kandeel, Mahmoud Asdaq, Syed Mohammed Basheeruddin Mohanlall, Viresh Al-Shari, Nizar A. Morsy, Mohamed A.
author	Venugopala, Katharigatta N.
author_facet	Venugopala, Katharigatta N. Shinu, Pottathil Tratrat, Christophe Deb, Pran Kishore Gleiser, Raquel M. Chandrashekharappa, Sandeep Chopra, Deepak Attimarad, Mahesh Nair, Anroop B. Sreeharsha, Nagaraja Mahomoodally, Fawzi M. Haroun, Michelyne Kandeel, Mahmoud Asdaq, Syed Mohammed Basheeruddin Mohanlall, Viresh Al-Shari, Nizar A. Morsy, Mohamed A.
author_role	author
author2	Shinu, Pottathil Tratrat, Christophe Deb, Pran Kishore Gleiser, Raquel M. Chandrashekharappa, Sandeep Chopra, Deepak Attimarad, Mahesh Nair, Anroop B. Sreeharsha, Nagaraja Mahomoodally, Fawzi M. Haroun, Michelyne Kandeel, Mahmoud Asdaq, Syed Mohammed Basheeruddin Mohanlall, Viresh Al-Shari, Nizar A. Morsy, Mohamed A.
author2_role	author author author author author author author author author author author author author author author author
dc.subject.none.fl_str_mv	ANOPHELES ARABIENSIS BIGINELLI REACTION CLICK CHEMISTRY IN SILICO DOCKING MOLECULAR HYBRIDIZATION MOSQUITO LARVICIDAL ACTIVITY PYRIMIDINE STEROL CARRIER PROTEIN-2 TRIAZOLE
topic	ANOPHELES ARABIENSIS BIGINELLI REACTION CLICK CHEMISTRY IN SILICO DOCKING MOLECULAR HYBRIDIZATION MOSQUITO LARVICIDAL ACTIVITY PYRIMIDINE STEROL CARRIER PROTEIN-2 TRIAZOLE
purl_subject.fl_str_mv	https://purl.org/becyt/ford/1.6 https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv	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; Sudáfrica. King Faisal University; Arabia Saudita Fil: Shinu, Pottathil. King Faisal University; Arabia Saudita Fil: Tratrat, Christophe. King Faisal University; Arabia Saudita Fil: Deb, Pran Kishore. Philadelphia University Jordan; Jordania Fil: Gleiser, Raquel M.. Universidad Nacional de Córdoba; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinar de Biología Vegetal (P). Grupo Vinculado Centro de Relevamiento y Evaluación de Recursos Agrícolas y Naturales; Argentina Fil: Chandrashekharappa, Sandeep. National Institute Of Pharmaceutical Education And Research, Raebareli; India Fil: Chopra, Deepak. Indian Institute Of Science Education And Research Bhopal; India Fil: Attimarad, Mahesh. King Faisal University; Arabia Saudita Fil: Nair, Anroop B.. King Faisal University; Arabia Saudita Fil: Sreeharsha, Nagaraja. Vidya Siri College Of Pharmacy; India. King Faisal University; Arabia Saudita Fil: Mahomoodally, Fawzi M.. University Of Mauritius; Mauricio Fil: Haroun, Michelyne. King Faisal University; Arabia Saudita Fil: Kandeel, Mahmoud. Faculty Of Veteinary Medicine; Egipto. King Faisal University; Arabia Saudita Fil: Asdaq, Syed Mohammed Basheeruddin. Almaarefa University; Arabia Saudita Fil: Mohanlall, Viresh. Durban University Of Technology; Sudáfrica Fil: Al-Shari, Nizar A.. Jordan University Of Science And Technology; Jordania Fil: Morsy, Mohamed A.. King Faisal University; Arabia Saudita. Faculty Of Medicine; Egipto
description	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.
publishDate	2022
dc.date.none.fl_str_mv	2022-05
dc.type.none.fl_str_mv	info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion http://purl.org/coar/resource_type/c_6501 info:ar-repo/semantics/articulo
format	article
status_str	publishedVersion
dc.identifier.none.fl_str_mv	http://hdl.handle.net/11336/200568 Venugopala, Katharigatta N.; Shinu, Pottathil; Tratrat, Christophe; Deb, Pran Kishore; Gleiser, Raquel M.; et al.; 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; Molecular Diversity Preservation International; Molecules; 27; 9; 5-2022; 1-16 1420-3049 CONICET Digital CONICET
url	http://hdl.handle.net/11336/200568
identifier_str_mv	Venugopala, Katharigatta N.; Shinu, Pottathil; Tratrat, Christophe; Deb, Pran Kishore; Gleiser, Raquel M.; et al.; 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; Molecular Diversity Preservation International; Molecules; 27; 9; 5-2022; 1-16 1420-3049 CONICET Digital CONICET
dc.language.none.fl_str_mv	eng
language	eng
dc.relation.none.fl_str_mv	info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules27092676 info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/1420-3049/27/9/2676
dc.rights.none.fl_str_mv	info:eu-repo/semantics/openAccess https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv	openAccess
rights_invalid_str_mv	https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv	application/pdf application/pdf
dc.publisher.none.fl_str_mv	Molecular Diversity Preservation International
publisher.none.fl_str_mv	Molecular Diversity Preservation International
dc.source.none.fl_str_mv	reponame:CONICET Digital (CONICET) instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str	CONICET Digital (CONICET)
collection	CONICET Digital (CONICET)
instname_str	Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv	CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv	dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_	1844613967416131584
score	13.070432

1,2,3-Triazolyl-tetrahydropyrimidine conjugates as potential Sterol Carrier Protein-2 Inhibitors: Larvicidal activity against the Malaria Vector Anopheles arabiensis and In Silico...

Publicaciones similares