title: Thiadiazole inhibitors: a patent review.
abstract: Four isomeric structures of thiadiazole motifs have outstanding pharmacological inhibitory applications are reported in this review. Thiadiazole nucleus is present in several biologically active natural products and commercial drugs. Most of thiadiazoles reported herein are emphasized to have broad spectrum of medicinal activities. Areas covered: This review represents the recent inhibitory activities of thiadiazole isomeric scaffolds and their broad-spectrum biological applications published as full texts during 2010-2016 as well as the patents published during 2005-2016. The inhibition areas covered included anti-inflammatory, antimicrobial, antitumor, antioxidant, antitubercular, antiviral, antileishmanial, anticonvulsant, herbicidal and algicidal activities in addition to enzymes, human platelet aggregation and neuroprotective inhibitors. Expert opinion: This survey revealed very interesting data about the applications of thiadiazoles, where some synthetic or natural thiadiazole derivatives were components of drugs available in the market. Many thiadiazole derivatives can be considered as lead compounds for drug synthesis. The most inhibitory active 1,3,4-thiadiazole compounds are those incorporating secondary alkyl(aryl)amido- and/or benzylthio(mercapto) groups at positions 2 and 5. Several thiadiazole derivatives demonstrated higher antibacterial, antitumor and antiviral activities than the standard drugs. Some thiadiazole derivatives exhibited high selective enzymes inhibitory activities based on the electronic properties of the substituents at positions 2 or 5.
authors.affiliation: a Department of Chemistry, Faculty of Science , Kuwait University , Safat , Kuwait.|b Department of Chemistry, Faculty of Science , Cairo University , Giza , Egypt.
authors.forename: Kamal M
authors.initials: KM
authors.lastname: Dawood
authors.affiliation: b Department of Chemistry, Faculty of Science , Cairo University , Giza , Egypt.|c Department of Chemistry, Faculty of Applied Science , Umm Al-Qura University , Makkah Almukkarramah , Saudi Arabia.
authors.forename: Thoraya A
authors.initials: TA
authors.lastname: Farghaly
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013830:Thiadiazoles
keywords: Anti-inflammatory; antimicrobial; antitumor; antiviral; enzymes inhibitors; thiadiazoles