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Chemical aspects of human and environmental overload with fluorine
Over the last 100–120 years, due to the ever-increasing importance of fluorine-containing
compounds in modern technology and daily life, the explosive development of the …
compounds in modern technology and daily life, the explosive development of the …
Fluorinated pyrazoles: From synthesis to applications
PK Mykhailiuk - Chemical Reviews, 2020 - ACS Publications
Fluorinated pyrazoles play an important role in medicinal chemistry, drug discovery,
agrochemistry, coordination chemistry, and organometallic chemistry. Since the early 1990s …
agrochemistry, coordination chemistry, and organometallic chemistry. Since the early 1990s …
The most common functional groups in bioactive molecules and how their popularity has evolved over time
The concept of functional groups (FGs), sets of connected atoms that can determine the
intrinsic reactivity of the parent molecule and in part are responsible for the overall …
intrinsic reactivity of the parent molecule and in part are responsible for the overall …
Applications of fluorine in medicinal chemistry
EP Gillis, KJ Eastman, MD Hill… - Journal of medicinal …, 2015 - ACS Publications
The role of fluorine in drug design and development is expanding rapidly as we learn more
about the unique properties associated with this unusual element and how to deploy it with …
about the unique properties associated with this unusual element and how to deploy it with …
Difluoromethyl bioisostere: examining the “lipophilic hydrogen bond donor” concept
Y Zafrani, D Yeffet, G Sod-Moriah… - Journal of Medicinal …, 2017 - ACS Publications
There is a growing interest in organic compounds containing the difluoromethyl group, as it
is considered a lipophilic hydrogen bond donor that may act as a bioisostere of hydroxyl …
is considered a lipophilic hydrogen bond donor that may act as a bioisostere of hydroxyl …
Good partnership between sulfur and fluorine: sulfur-based fluorination and fluoroalkylation reagents for organic synthesis
C Ni, M Hu, J Hu - Chemical Reviews, 2015 - ACS Publications
Fluorine, often called as “a small atom with a big ego”, 1 lies in the second row and the 17th
column in the periodic table of the chemical elements. This unique position in the periodic …
column in the periodic table of the chemical elements. This unique position in the periodic …
Fluorinated cycloalkyl building blocks for drug discovery
OO Grygorenko, KP Melnykov, S Holovach… - …, 2022 - Wiley Online Library
The review covers various aspects of fluorinated cycloalkyl (C3− C7) building blocks for drug
discovery, including their synthesis, key physicochemical properties, and biological and …
discovery, including their synthesis, key physicochemical properties, and biological and …
Fluorine in medicinal chemistry
S Swallow - Progress in medicinal chemistry, 2015 - Elsevier
Since its first use in the steroid field in the late 1950s, the use of fluorine in medicinal
chemistry has become commonplace, with the small electronegative fluorine atom being a …
chemistry has become commonplace, with the small electronegative fluorine atom being a …
Effect of gem‐Difluorination on the Key Physicochemical Properties Relevant to Medicinal Chemistry: The Case of Functionalized Cycloalkanes
S Holovach, KP Melnykov… - … A European Journal, 2022 - Wiley Online Library
Physico‐chemical properties important to drug discovery (pKa, LogP, and aqueous
solubility), as well as metabolic stability, were studied for a series of functionalized gem …
solubility), as well as metabolic stability, were studied for a series of functionalized gem …
Discovery of 4-((3′R,4′S,5′R)-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5 …
A Aguilar, J Lu, L Liu, D Du, D Bernard… - Journal of medicinal …, 2017 - ACS Publications
We previously reported the design of spirooxindoles with two identical substituents at the
carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper we describe an …
carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper we describe an …