Trimethoprim is currently often utilized in modern medicine due to its organic features. ‎‎Trimethoprim inhibits vulnerable organisms from converting dihydrofolate to ‎tetrahydrofolate, which is the active form of Folic acid.‎ We report on many Trimethoprim ‎derivatives and their complexes were characterized using various spectroscopic techniques, ‎including X-ray diffraction, infrared, and ultraviolet-visible measurements.‎ In this review, ‎the pharmacological properties and molecular mechanism of TMP in recent years are ‎discussed. Trimethoprim derivatives are created when their molecular composition is ‎modified, increasing the probability that they will bind to proteins. Trimethoprim is a ‎bridging bidentate ligand that can bind to metal ions via its amino groups and pyrimidine ‎rings. This review outlines a decade of study on the biological properties of trimethoprim ‎derivatives. Trimethoprim derivatives have been shown to exhibit several biological ‎characteristics throughout the last few decades. With great therapeutic results, it has been ‎utilized to treat a wide range of diseases. Therefore, it is a promising drug with a lot of ‎scope for study. ‎