Novel hybrids of fluconazole and furanones: Design, synthesis and antifungal activity

Antifungal activity of synthetic naphthoquinones against dermatophytes and opportunistic fungi: preliminary mechanism-of-action tests

“…The recent high incidence of fungal infections is due to the increased number of immunocompromised patients who are infected with HIV or have undergone organ transplantation or chemotherapy [1]. Although effective antifungal agents are currently available, side effects such as toxicity, drug interactions, inadequate pharmacokinetic properties and the development of resistance have been reported [2].…”

The Drug Discovery and Development Industry in India—Two Decades of Proprietary Small‐Molecule R&D

“…manufactures and sells APIs and formulations, and initiated efforts in R&D around 2000, focusing on academic collaborations, in particular with the National Chemical Laboratory (NCL) in Pune, on antifungals, which has led to a series of joint patent applications, including on Fluconazole analogues 32, 149, 150, 151, 152. No progress, however, has been reported on NCL‐FDC‐101, an early‐stage compound disclosed in 2006, which is likely to have been abandoned, as no reference has been made to drug discovery in annual reports since 2013 (Supporting Information Table 6a, entry 104) 149…”

“…[148] FDC Ltd. manufactures and sells APIs and formulations, and initiated efforts in R&D around2000, focusing on academic collaborations, in particularwith the National Chemical Laboratory (NCL) in Pune, on antifungals, which has led to as eries of joint patent applications,i ncluding on Fluconazole analogues. [32,[149][150][151][152] No progress, however,h as been reported on NCL-FDC-101, an early-stage compound disclosed in 2006, which is likely to have been abandoned, asn or eference has been made to drug discovery in annualr eports since 2013 (Supporting Information Ta ble 6a, entry 104). [149] JB Chemicals &P harmaceuticals Ltd. (JBCPL),ap roducer of generics and bulk drugs established in 1976, initiated NCE research around the year 2000, working on NSAIDS including cyclooxygenase-2 (COX-2) inhibitors for the treatment of inflammation; [32,[153][154][155] In 2004 the company reportedt hree compounds in preclinical development, including JB-7/G (Supporting Information Ta ble 6a, entry 105).…”

Synthesis of highly substituted γ-hydroxybutenolides through the annulation of keto acids with alkynes and subsequent hydroxyl transposition

“…The construction of a five-membered lactone is the key step in the synthesis of g-hydroxybutenolides, and has made great progress in the past few decades. Among these methods, there are two common strategies: (a) intermolecular aldol reaction between a-bromoketone and acetic acid followed by air oxidation (Scheme 1, eqn (1)), [4][5][6][7][8] and (b) aldol condensation between g-ketoesters and aldehydes (Scheme 1, eqn (2)). 9-14 However, the former requires the use of preformed perishable a-bromoketones and the latter harnesses the multi-step prepared g-ketoesters which are sometimes hard to make.…”