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Trimethoprim and Trimethoprim–Sulfamethoxazole (Cotrimoxazole)
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Jason A. Trubiano, M. Lindsay Grayson
At least one new diaminopyrimidine has been developed, iclaprim, which appears to retain activity against some TMP-resistant Gram-positive bacteria (Schneider et al., 2003; Laue et al., 2007), but there are only limited clinical efficacy data such that development appears to have stalled (see Chapter 96, Iclaprim).
Trimethoprim-Sulfamethoxazole
Published in Thomas T. Yoshikawa, Shobita Rajagopalan, Antibiotic Therapy for Geriatric Patients, 2005
Stephen Marer, Shobita Rajagopalan
Trimethoprim is a diaminopyrimidine that competitively inhibits dihydrofolate reductase. Dihydrofolate reductase catalyzes the conversion of folic acid into tetra-hydrofolic acid, the most active form of folic acid. Trimethoprim is highly selective for dihydrofolate reductase of lower organisms, thus leaving the crucial enzymatic step intact in mammalian cells (2). By itself, trimethoprim is bacteriostatic or weakly bactericidal. However, by inhibiting sequential steps in the formation of tetrahyro-folic acid, the combination of sulfonamides with trimethoprim is often synergistic and therefore bactericidal.
Dihydrofolate reductase inhibitors: patent landscape and phases of clinical development (2001–2021)
Published in Expert Opinion on Therapeutic Patents, 2022
Kavita Bhagat, Nitish Kumar, Harmandeep Kaur Gulati, Aanchal Sharma, Amandeep Kaur, Jatinder Vir Singh, Harbinder Singh, Preet Mohinder Singh Bedi
MTX exhibited good DHFR inhibitory activity due to the presence of glutamate moiety that helps in transportation and retention inside the cells. In 2011, Chen et al. filed a patent on diaminoquinazolines derivatives (Table 2) and also describing various methods of assessing DHFR inhibitory activity. These derivatives were beneficial for the treatment of numerous diseases such as inflammatory diseases including both bacterial and fungal infections, cell proliferative diseases, and autoimmune diseases. The antibacterial activity of all the synthetics was carried out by using a whole-cell bacterial growth inhibition assay. Results of the assay indicate that compound 8 showed inhibitory activity against S. aureus bacterial strain with MIC value ≤ 0.125 µg/mL. From the above results, it can be concluded that compounds with diaminopyrimidine ring could be beneficial for humanity to treat various bacterial, proliferative, and autoimmune diseases [66].
Current and future treatment options for community-associated MRSA infection
Published in Expert Opinion on Pharmacotherapy, 2018
A. Khan, B. Wilson, I. M. Gould
Iclaprim is a diaminopyrimidine that inhibits bacterial dihydrofolate reductase [160]. It has potent activity against gram-positive organisms and exhibits bactericidal activity against MRSA [160]. A recently published phase 3 study has demonstrated Iclaprim non-inferiority to vancomycin in the treatment of ABSSSI caused by gram-positive organisms, including MRSA, with no significant adverse events secondary to treatment [161].
Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasi
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Bárbara Velame Ferreira Teixeira, André Lacerda Braga Teles, Suellen Gonçalves da Silva, Camila Carane Bitencourt Brito, Humberto Fonseca de Freitas, Acássia Benjamim Leal Pires, Thamires Quadros Froes, Marcelo Santos Castilho
The 2,4-diaminopyrimidine derivatives were synthesized as described by Teles et al.27. Briefly, all compounds were obtained in moderate yields by the condensation of suitable ketonitriles and guanidine as described in Figure 1.