3D-FD63748 - diphenylhydramine-related-compound-b

Chloroquine

Diphenhydramine

N4-(7-Chloroquinolin-4-Yl)-N1,N1-Diethylpentane-1,4-Diamine

Diphenhydramine

Diphenhydramine (Syntedril): first-gen antihistamine for allergies, antiemetic, antitussive, anticholinergic, sedative, treats drug-induced parkinsonism.

Chloroquine: antimalarial, anti-inflammatory, autophagy/TLRs inhibitor, treats arthritis, effective against COVID-19 in vitro. EC50: 1.13 μM.

Chloroquine is a 4-aminoquinolone that is used to prevent and treat malaria, caused by parasitic protozoan from the Plasmodium genus. Chloroquine is are an schizonticidal agent and is a widely prescribed antimalarial compound. The antiviral activity of chloroquine in vitro has been reported in 1960’s and recent publications have brought attention to its possible benefits in the treatment of COVID-19 patients, infected with the newly emerged coronavirus (SARS-CoV-2). Current evidence shows that chloroquine inhibits SARS CoV-2 entry in host cells by interfering with endocytosis and the glycoprofile on the S-glycoprotein.

Diphenhydramine is a drug that belongs to the class of antihistamines, and is used to treat allergic symptoms such as hay fever, urticaria, and other allergic reactions. It has been shown to inhibit the production of hydrogen fluoride in analytical methods for measuring this compound. Diphenhydramine is also known to have potential interactions with other drugs, including α1-adrenergic antagonists (i.e., h1-antagonists), cyclic peptides, and surfactants. In addition, it has been shown to bind to the α1 subunit of G protein receptors within the gastrointestinal tract in a reaction mechanism that is not yet fully understood. This binding inhibits the response of these receptors to certain stimuli from neurotransmitters and hormones, which can lead to bowel disease.