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About the Authors:
Polina V. Oliferenko
Affiliation: Department of Chemistry, University of Florida, Gainesville, Florida, United States of America
Alexander A. Oliferenko
Affiliation: Department of Chemistry, University of Florida, Gainesville, Florida, United States of America
Gennadiy I. Poda
Affiliation: Medicinal Chemistry Platform, Ontario Institute for Cancer Research, Toronto, Ontario, Canada
Dmitry I. Osolodkin
Affiliation: Department of Chemistry, Lomonosov Moscow State University, Moscow, Russia
Girinath G. Pillai
Affiliations Department of Chemistry, University of Florida, Gainesville, Florida, United States of America, Institute of Chemistry, University of Tartu, Tartu, Estonia
Ulrich R. Bernier
* E-mail: [email protected] (ARK); [email protected] (URB)
Affiliation: USDA-ARS-CMAVE, Gainesville, Florida, USA
Maia Tsikolia
Affiliation: USDA-ARS-CMAVE, Gainesville, Florida, USA
Natasha M. Agramonte
Affiliation: USDA-ARS-CMAVE, Gainesville, Florida, USA
Gary G. Clark
Affiliation: USDA-ARS-CMAVE, Gainesville, Florida, USA
Kenneth J. Linthicum
Affiliation: USDA-ARS-CMAVE, Gainesville, Florida, USA
Alan R. Katritzky
* E-mail: [email protected] (ARK); [email protected] (URB)
Affiliations Department of Chemistry, University of Florida, Gainesville, Florida, United States of America, Chemistry Department, King Abdulaziz University, Jeddah, Saudi Arabia
Introduction
Natural sources, such as local herbs and gum, oil and plant-based smoke, have been used by mankind for millennia as mosquito repellents and are still utilized today by 50-90% of residents throughout the rural tropics [1]. Intensive research to discover more effective, long-lasting, and water-resistant repellents began during WWII because of more than one million cases of malaria recorded among the U.S. troops involved in overseas campaigns [1]. The most effective wide-spectrum synthetic repellent to emerge from this program was N,N-diethyl-3-methylbenzamide (DEET) (see Figure 1) discovered in 1952.
Although considered a gold standard for insect repellents, DEET does have disadvantages: (i) limited efficacy against Anopheles albimanus (the principal malaria vector in Central America and the Caribbean) [2], tolerant varieties of Aedes aegypti [3], and some other vectors [4] (ii) skin irritation; (iii) possible neurotoxicity [5]; (iv) a plasticising action on polymeric materials; and (v) relatively high cost. Additional repellent active ingredients (Figure 1) such as the piperidine derivatives KBR 3023 (picaridin) and AI3-37220 are considered almost as efficacious as DEET, and in some cases reported to remain effective for a longer duration and have more desirable cosmetic properties. The repellent diethyl phenylacetamide (DEPA) is as reported to be as efficacious as DEET and can be produced at about half the cost of...