Recent advances of imidazole-containing derivatives as anti-tubercular agents

YL Fan, XH Jin, ZP Huang, HF Yu, ZG Zeng… - European journal of …, 2018 - Elsevier
Tuberculosis still remains one of the most common, communicable, and leading deadliest
diseases known to mankind throughout the world. Drug-resistance in Mycobacterium …

Revealing quinquennial anticancer journey of morpholine: A SAR based review

F Arshad, MF Khan, W Akhtar, MM Alam… - European journal of …, 2019 - Elsevier
Morpholine, a six-membered heterocycle containing one nitrogen and one oxygen atom, is a
moiety of great significance. It forms an important intermediate in many industrial and …

Oxazolidinones as versatile scaffolds in medicinal chemistry

GFS Fernandes, CB Scarim, SH Kim, J Wu… - RSC Medicinal …, 2023 - pubs.rsc.org
Oxazolidinone is a five-member heterocyclic ring with several biological applications in
medicinal chemistry. Among the three possible isomers, 2-oxazolidinone is the most …

Recent advancements and developments in search of anti-tuberculosis agents: a quinquennial update and future directions

TM Dhameliya, KA Bhakhar, ND Gajjar, KA Patel… - Journal of Molecular …, 2022 - Elsevier
Tuberculosis (TB) has been considered as the highly chronic, contagious and infectious
disorder caused by Mycobacterium tuberculosis (Mtb). Every year more than 10 million …

Thiophene‐containing compounds with antimicrobial activity

G Roman - Archiv der Pharmazie, 2022 - Wiley Online Library
Thiophene, as a member of the group of five‐membered heterocycles containing one
heteroatom, is one of the simplest heterocyclic systems. Many synthetic strategies allow the …

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist

SL Degorce, MS Bodnarchuk… - ACS Medicinal Chemistry …, 2019 - ACS Publications
We have conducted an analysis of azaspiro [3.3] heptanes used as replacements for
morpholines, piperidines, and piperazines in a medicinal chemistry context. In most cases …

Design, synthesis and biological evaluation of novel spiro-quinazolinone derivatives as chitin synthase inhibitors and antifungal agents

C Du, X Yang, Y Long, X Lang, L Liu, Y Xu… - European Journal of …, 2023 - Elsevier
A series of spiro-quinazolinone scaffolds were constructed based on the bioactivity of
quinazolinone and the inherent feature of spirocycle to design novel chitin synthase …

Practical and Scalable Two-Step Process for 6-(2-Fluoro-4-nitrophenyl)-2-oxa-6-azaspiro [3.3] heptane: A Key Intermediate of the Potent Antibiotic Drug Candidate TBI …

FSP Cardoso, AL Kadam, RC Nelson… - … Process Research & …, 2023 - ACS Publications
A low-cost, protecting group-free route to 6-(2-fluoro-4-nitrophenyl)-2-oxa-6-azaspiro [3.3]
heptane (1), the starting material for the in-development tuberculosis treatment TBI-223, is …

Design, synthesis and biological evaluations of quinolone amides against African trypanosomiasis with improved solubility

J Weinmann, L Kirchner, M Engstler, L Meinel… - European Journal of …, 2023 - Elsevier
The human African trypanosomiasis is a devastating parasitic infection, which is caused by
the protozoan Trypanosoma brucei and transmitted by the bite of the tsetse fly. An untreated …

Design, synthesis and biological evaluation of 2, 3-dihydroimidazo [2, 1-b] thiazoles as dual EGFR and IGF1R inhibitors

PK Gadekar, G Urunkar, A Roychowdhury… - Bioorganic …, 2021 - Elsevier
Herein we describe the design, synthesis and anticancer evaluation of a series of 2, 3-
dihydroimidazo [2, 1-b] thiazoles as dual kinase inhibitors of IGF1R and EGFR. A series of …