Natural Indole Alkaloids from Marine Fungi: Chemical Diversity and Biological Activities

Li, Jiao; Zhuang, Chun-Lin

This review attempts to provide a summary of the structural diversity of marine fungal indole alkaloids as well as their known biological activities. A total of 306 indole alkaloids from marine fungi have been summarized, covering the references published from 1995 to early 2021, expecting to be beneficial for drug discovery in the future.

Metal Complexes as DNA Synthesis and/or Repair Inhibitors: Anticancer and Antimicrobial Agents

Ngoepe, Mpho Phehello; Clayton, Hadley S.

DNA adduct formation with metal complex: (A) monoadduct, (B) protein-DNA, (C) 1,3-intrastrand, (D)1,2-intrastrand and inter-strand crosslink.

DNA and RNA are ideal drug targets for therapeutic intervention in the case of various diseases, such as cancer and microbial infection. The review summarized various interactions of metal complexes with DNA nucleic acids, as well as the underlying mechanisms of action. Furthermore, the review also highlighted various tools that are used to investigate the interaction.

Design, Synthesis, and Antidepressant Activity Study of Novel Aryl Piperazines Targeting Both 5-HT_1A and Sigma-1 Receptors

Yan-Na Ni, Xin-Li Du, Tao Wang, Yuan-Yuan Chen, Xiang-Qing Xu, Song Zhao, Jian-Qi Li, Guan Wang

A total of 20 novel aryl piperazine derivatives (compound 11-30) were designed and synthesized using OPC-14523 as the lead compound. Among those derivatives, compound 27 showed high affinity for 5-HT1A and σ1 receptors, exhibited good antidepressant activity, and had good metabolic stability, PK characteristics and low acute toxicity. Compound 27 may represent a promising active molecule for depression therapy in the further.

Enantioselective aza-Michael Cyclization Reaction Catalyzed by Quinine-Derived Monoquaternary Ammonium Salts: an Effective Route to Synthesize Letermovir

Liang Chen, Wei-Yuan Liu, Si-Ju Bi, Ting Zhou, Jing Pan, Xun-Lei Lv, Kuai-Le Lin, Wei-Cheng Zhou

The optimal catalyst Q1 (quinine-derived monoquaternary ammonium salt) was explored as potent PTC for the reactionof aza-Michael cyclization, the key step in the synthesis of letermovir (1). PTC Q1 is preferred, due to its good enantioselectivity, easy preparation from cheap material, as well as the possibility of reuse. With the optimal catalyst Q1 in hand, the synthesis of letermovir would be more convenient and economical. PTC, phase-transfer catalyst.

Enhancement of Aqueous Solubility, Dissolution Profile, and Oral Bioavailability of Pentoxifylline by Microsponges

Anil Raosaheb Pawar, Nikhil Arun Shete, Priyanka Vitthal Jadhav, Vinayak Kashinath Deshmukh, Jaswandi Sameer Mehetre

The work suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile and oral bioavailability of pentoxifylline.