Drug intelligence / Profile preview

2-amino-1,3,4-thiadiazole

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intramuscular, Parenteral, Topical, Rectal
01

Overview

2-amino-1,3,4-thiadiazole (NSC 4728) is a chemical compound that has been investigated for its antineoplastic properties. It functions as a potent inhibitor of inosine 5'-phosphate (IMP) dehydrogenase, with its metabolite, aminothiadiazole mononucleotide, acting as a competitive inhibitor of IMP. Clinical studies in the 1980s evaluated its use in various cancers, demonstrating some antitumor responses in lung, esophageal, cervical, and renal cell carcinomas. Common side effects observed included stomatitis, dermatitis, nausea, vomiting, lethargy, and hyperuricemia. Beyond its anticancer research, derivatives of 2-amino-1,3,4-thiadiazole have been explored for their potential antimicrobial (antibacterial, antifungal, antitubercular) and antiviral activities, highlighting the broad pharmacological interest in this chemical scaffold.

Other names
aminothiadiazole
02

Targets

DNAQPCT (Glutaminyl-peptide cyclotransferase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)QPCTL (Iso-glutaminyl cyclase)PTGES (Microsomal prostaglandin E synthase-1)TbPTR1 (Trypanosoma brucei pteridine reductase 1)

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